Ranitidine

别名: ranitidine; 66357-35-5; Ranitidine Base; ranitidine hydrochloride; Raticina; Coralen; Gastrial; Quantor; 雷尼替丁; 呋喃硝胺; 甲硝呋;雷尼替丁碱;呋硫硝胺;甲硝呋胍;善胃得;胃安太定;善得胃;胃安太;盐酸雷尼替丁;N'-甲基-N-[2-[[[5-[(二甲氨基)甲基]-2-呋喃基]-甲基]硫代]乙基]-2-硝基-1,1-乙烯二胺盐酸盐
目录号: V10991 纯度: ≥98%
雷尼替丁是一种强效、选择性、口服生物活性组胺 H2 受体阻滞剂(拮抗剂),IC50 为 3.3 μM,可抑制胃液分泌。
Ranitidine CAS号: 66357-35-5
产品类别: New1
产品仅用于科学研究,不针对患者销售
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Other Forms of Ranitidine:

  • 盐酸雷尼替丁
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产品描述
雷尼替丁是一种强效、选择性、口服生物活性的组胺H2受体阻滞剂(拮抗剂),IC50值为3.3 μM,可抑制胃酸分泌。雷尼替丁也是CYP2C19和CYP2C9的弱抑制剂。
雷尼替丁(CAS号:66357-35-5)是一种组胺H2受体拮抗剂,曾广泛用于治疗消化性溃疡、胃食管反流病(GERD)和卓-艾综合征。其作用机制是减少胃酸分泌。在质子泵抑制剂广泛应用之前,雷尼替丁是治疗酸相关疾病最常用的药物之一。它有多种剂型,包括片剂、泡腾片和口服溶液。
生物活性&实验参考方法
靶点
Histamine H2 receptor
Ranitidine targets the histamine H2 receptor on gastric parietal cells. By binding to and blocking the H2 receptor, ranitidine inhibits the action of histamine, which is a major stimulus for gastric acid secretion. This leads to a reduction in the volume and acidity of gastric juice. Ranitidine's inhibition of acid secretion is dose-dependent and reversible.
体外研究 (In Vitro)
体外活性:雷尼替丁可增加肝细胞对活化中性粒细胞产生的细胞毒性产物的敏感性,而甲硝唑则无此作用。[1] 当脂多糖用于体外刺激单核细胞时,雷尼替丁可抑制肿瘤坏死因子-α (TNF-α) 的产生。雷尼替丁[2] 可提高分离的豚鼠肝细胞中吗啡-6-葡萄糖醛酸苷与吗啡-3-葡萄糖醛酸苷的相对浓度,并呈剂量依赖性地降低吗啡的Kel值,最大效应达50%。雷尼替丁可使吗啡-3-葡萄糖醛酸苷/吗啡-6-葡萄糖醛酸苷的比值逐渐降低,最高可达21%。[3]
体外研究表明,雷尼替丁可抑制组胺刺激的分离壁细胞和胃黏膜制剂中的胃酸分泌。该化合物通过竞争性抑制作用阻断组胺与H2受体的结合。雷尼替丁已被证明是多种体外模型中强效的胃酸分泌抑制剂,其IC50值在纳摩尔范围内。
体内研究 (In Vivo)
雷尼替丁可导致肝损伤,表现为大鼠服用雷尼替丁6小时后血清中γ-谷氨酰转移酶、天冬氨酸氨基转移酶和丙氨酸氨基转移酶水平升高。[1] 雷尼替丁可抑制细胞因子诱导的中性粒细胞趋化因子、中性粒细胞在肝脏的聚集以及由大鼠肝脏缺血/再灌注引起的肝组织中TNF-α水平升高。[2] 在接受LPS和雷尼替丁治疗的大鼠中,抗凝剂可减轻肝损伤,而雷尼替丁联合治疗则会增加LPS诱导的凝血作用,从而在肝损伤发生前增强凝血。接受雷尼替丁或LPS治疗的大鼠肝窦内会形成纤维蛋白凝块,并且由于纤维蛋白沉积受到抑制,因此发生肝细胞损伤的可能性较低。在大鼠中,雷尼替丁联合治疗可增强LPS诱导的TNF升高,且在肝细胞损伤出现之前即可观察到。[4]
体内研究表明,雷尼替丁能有效减少人和动物的胃酸分泌。临床研究证实其对治疗十二指肠溃疡、胃溃疡和糜烂性食管炎有效。雷尼替丁还被证实能有效预防溃疡复发和治疗卓-艾综合征。该化合物起效迅速,并能持续抑制胃酸分泌。
酶活实验
雷尼替丁的体外受体结合试验通常包括使用放射性配体结合法测定其与组胺H2受体的亲和力。将化合物与表达H2受体的细胞膜制备物以及放射性标记的配体(例如[3H]噻替丁)一起孵育。测定置换50%放射性配体所需的雷尼替丁浓度(IC50),并计算Ki值。由此可以评估雷尼替丁对H2受体相对于H1和H3受体的选择性。
细胞实验
本研究在离体豚鼠肝细胞中探讨了雷尼替丁对吗啡代谢的影响,尤其关注吗啡-3-葡萄糖醛酸苷与吗啡-6-葡萄糖醛酸苷的比例。结果表明,雷尼替丁呈剂量依赖性地降低了吗啡的Kel值,最大效应达50%,并提高了吗啡-6-葡萄糖醛酸苷与吗啡-3-葡萄糖醛酸苷的相对浓度。这些效应可能是由于雷尼替丁对相关结合酶的直接或间接作用,或对吗啡或葡萄糖醛酸苷跨细胞膜转运的影响所致。然而,后一种解释被否定,因为雷尼替丁并未影响细胞内和细胞外吗啡、吗啡-3-葡萄糖醛酸苷和吗啡-6-葡萄糖醛酸苷的浓度比值。随着雷尼替丁浓度的增加,吗啡-3-葡萄糖醛酸苷/吗啡-6-葡萄糖醛酸苷的比值逐渐降低,最高可达21%。这可能是由于能量或辅底物供应受到干扰,或直接作用于不同的UDP-葡萄糖醛酸转移酶所致。观察到雷尼替丁对吗啡葡萄糖醛酸化的影响与使用已知辅底物(UDPGA)耗竭剂时观察到的影响相反,这表明雷尼替丁的作用很可能是直接抑制相关的尿苷5'-二磷酸葡萄糖醛酸转移酶,并且对负责3'-葡萄糖醛酸化的同工酶的影响更为显著。[3]
体外细胞实验中,雷尼替丁通常用于培养壁细胞或表达H2受体的细胞系。细胞用不同浓度的雷尼替丁处理,并用组胺刺激。测量组胺诱导的胃酸分泌或cAMP积累的抑制情况。抑制这些反应的IC50值由剂量反应曲线确定。雷尼替丁对细胞活力和受体内化的影响也可进行评估。
动物实验
药物特异反应是指少数服用某种药物的人群中发生的病因不明的不良反应。某些特异反应可能由药物肝毒性阈值的间歇性降低引起。既往大鼠研究表明,由细菌脂多糖 (LPS) 诱发的轻度炎症可降低异源物质肝毒性阈值。组胺-2 (H2) 受体拮抗剂雷尼替丁 (RAN) 可引起人类特异反应,肝脏通常是其靶器官。研究人员检验了以下假设:在经历轻度炎症反应的动物中,RAN 可能具有肝毒性。[1]
雄性大鼠接受非肝毒性剂量的 LPS(44 x 10⁶ 内毒素单位/kg,静脉注射)或其溶剂,2 小时后接受非肝毒性剂量的 RAN(30 mg/kg,静脉注射)或其溶剂。仅在同时接受雷帕霉素(RAN)和脂多糖(LPS)治疗的动物中观察到肝损伤,表现为RAN给药后6小时内血清丙氨酸氨基转移酶(ALT)、天冬氨酸氨基转移酶(AST)和γ-谷氨酰转移酶(GGT)活性升高。LPS/RAN联合治疗导致肝脏中部出现病变,其特征为急性坏死性化脓性肝炎。法莫替丁(FAM)是一种H2受体拮抗剂,其特异性反应的发生率远低于RAN。给予大鼠与RAN药理效力相当的LPS和FAM后,未观察到肝损伤。体外实验表明,RAN可使肝细胞对活化中性粒细胞产生的细胞毒性产物更加敏感,而FAM则不具备这种能力。结果表明,在轻度炎症期间,动物暴露于雷尼替丁(RAN)可重现类似于人类雷尼替丁特异性反应的症状。[1]
此前有研究报道,H₂受体拮抗剂雷尼替丁可在体外和体内抑制中性粒细胞活化,从而有助于减轻大鼠应激诱导的胃黏膜损伤。本研究旨在探讨雷尼替丁是否能减轻大鼠缺血/再灌注引起的肝损伤(活化的中性粒细胞在其中起着关键作用)。此外,研究人员还考察了另一种H₂受体拮抗剂法莫替丁对体外和缺血/再灌注引起的肝损伤后大鼠白细胞活化的影响,以探究雷尼替丁对中性粒细胞活化的抑制作用是否依赖于其对H₂受体的阻断。如先前报道,雷尼替丁在体外抑制了中性粒细胞的活化,而法莫替丁则显著增强了中性粒细胞的活化。雷尼替丁可抑制脂多糖体外刺激的单核细胞中肿瘤坏死因子-α (TNF-α) 的产生,而法莫替丁则无此作用。尽管静脉注射30 mg/kg雷尼替丁可抑制肝脏缺血/再灌注引起的肝组织中TNF-α水平升高、细胞因子诱导的中性粒细胞趋化因子水平升高以及中性粒细胞在肝脏中的聚集,但静脉注射5 mg/kg法莫替丁却显著增强了这些升高。雷尼替丁可显著抑制再灌注后肝组织血流量和胆汁分泌的减少以及血清转氨酶水平的升高,而法莫替丁组动物的这些变化比对照组更为显著。这些观察结果强烈提示,雷尼替丁可通过直接抑制中性粒细胞活化,或通过抑制中性粒细胞强效活化剂TNF-α的产生而间接抑制中性粒细胞活化,从而减轻缺血/再灌注引起的肝损伤。此外,雷尼替丁的治疗效果可能并非仅仅由其对H₂受体的阻断作用所致。[2] 雷尼替丁的体内动物研究通常在啮齿动物或犬模型中进行,以评估其对胃酸分泌的影响。该化合物可通过口服或静脉注射给药。胃酸分泌的测量方法包括收集胃内容物或使用胃瘘。研究评估雷尼替丁对基础和刺激性胃酸分泌的影响。此外,还需进行药代动力学研究,以评估该化合物的吸收、分布和消除情况。
药代性质 (ADME/PK)
代谢/代谢物
雷尼替丁的已知代谢物包括去甲基雷尼替丁。
雷尼替丁是一种药代动力学特性明确的药物。口服后,它能迅速从胃肠道吸收。雷尼替丁的生物利用度约为50%。它在肝脏代谢为多种代谢物。消除半衰期约为2-3小时。雷尼替丁主要以代谢物的形式经尿液排泄。
毒性/毒理 (Toxicokinetics/TK)
妊娠期和哺乳期影响
◉ 哺乳期用药概述
尽管个体差异较大,但母乳中的雷尼替丁剂量低于新生儿用药剂量。然而,由于发现雷尼替丁会自发分解成致癌化学物质,因此已在美国和其他一些国家撤市。建议使用替代药物。
◉ 对母乳喂养婴儿的影响
一位母亲连续两天每12小时服用150毫克雷尼替丁,之后她所哺乳的54天大的婴儿未观察到不良反应。
◉ 对哺乳和母乳的影响
已知组胺H2受体拮抗剂会刺激催乳素分泌。一些研究表明,静脉注射超过100毫克雷尼替丁或长期口服雷尼替丁会导致血清催乳素水平升高,罕见情况下会出现男性乳房发育症。对于已建立泌乳的母亲而言,催乳素水平可能不会影响其哺乳能力。
雷尼替丁是一种经临床批准的药物,具有良好的安全性。最常见的不良反应较轻,包括头痛、头晕、便秘和腹泻。罕见但严重的不良反应包括肝毒性、心律失常和血液疾病。2019年,由于在雷尼替丁产品中检测到N-亚硝基二甲胺(NDMA,一种可能的人类致癌物),雷尼替丁在许多国家被撤出市场。
参考文献

[1]. J Pharmacol Exp Ther. 2003 Oct;307(1):9-16.

[2]. J Pharmacol Exp Ther. 2002 Jun;301(3):1157-65.

[3]. Pharmacol Toxicol. 1998 Jun;82(6):272-9.

[4]. Toxicol Sci. 2007 Nov;100(1):267-80.

[5]. Neuropharmacology. 1998 Aug;37(8):1019-32.

其他信息
雷尼替丁属于呋喃类药物,用于治疗消化性溃疡和胃食管反流病。它具有多种作用,包括抗溃疡、拮抗H2受体、对抗环境污染物、外源性物质和药物过敏原。雷尼替丁属于呋喃类化合物、叔胺类化合物、C-硝基化合物和有机硫化合物。雷尼替丁是一种具有抗酸活性的组胺H2受体拮抗剂。雷尼替丁是肠嗜铬样细胞(ECL细胞)释放的组胺与胃壁细胞上的组胺H2受体结合的竞争性可逆抑制剂,从而抑制正常胃酸分泌和食物摄入引起的胃酸分泌。此外,当H2受体被阻断时,其他促进胃酸分泌的物质对胃壁细胞的作用也会减弱。盐酸雷尼替丁属于组胺H2受体拮抗剂类药物。雷尼替丁是一种竞争性、可逆性组胺抑制剂,可抑制肠嗜铬样细胞(ECL细胞)释放的组胺,并与胃壁细胞上的组胺H2受体结合,从而抑制正常的胃酸分泌和食物诱导的胃酸分泌。此外,当H2受体被阻断时,其他促进胃酸分泌的物质对胃壁细胞的作用也会减弱。雷尼替丁是一种非咪唑类组胺受体(H2受体)阻滞剂,可调节胃酸分泌。它用于治疗胃肠道溃疡。另见:雷尼替丁(注:已移至此处)。接触非毒性剂量的细菌脂多糖(LPS)会增加组胺H2受体拮抗剂雷尼替丁(RAN)的肝毒性。由于脂多糖(LPS)相关的某些病理生理效应是通过肿瘤坏死因子-α(TNF)等炎症介质的表达和释放介导的,本研究旨在了解TNF在LPS/雷帕霉素(RAN)肝毒性中的作用。为了确定雷帕霉素(RAN)是否影响LPS诱导的肝损伤早期TNF的释放,我们用2.5 × 10⁶内毒素单位(EU)/kg LPS或其生理盐水(静脉注射)处理雄性Sprague-Dawley大鼠,2小时后再用30 mg/kg RAN或无菌磷酸盐缓冲液(静脉注射)处理。LPS给药导致循环TNF浓度升高。RAN联合治疗增强了LPS诱导的TNF升高,且这种升高发生在肝细胞损伤之前,而法莫替丁(一种非特异性H2受体拮抗剂)则没有这种作用。血清白细胞介素 (IL)-1β、IL-6 和 IL-10 也观察到了类似的改变。为了确定 TNF 是否在 LPS/RAN 诱导的肝毒性中起因果作用,研究人员分别给大鼠静脉注射己酮可可碱 (PTX; 100 mg/kg) 以抑制 TNF 合成,或皮下注射依那西普 (Etan; 8 mg/kg) 以阻断 TNF 与细胞受体的结合,随后进行 LPS 和 RAN 处理。研究人员评估了肝细胞损伤、炎症介质的释放、肝脏中性粒细胞 (PMN) 聚集以及凝血和纤溶生物标志物。结果表明,PTX 或 Etan 预处理可减轻 LPS/RAN 联合处理动物的肝损伤,并降低循环中 TNF、IL-1β、IL-6、巨噬细胞炎症蛋白-2 以及凝血/纤溶生物标志物的浓度。然而,PTX 或 Etan 预处理均未改变肝脏 PMN 聚集。这些结果表明,TNF 通过增强炎症细胞因子的产生和止血作用来促进 LPS/RAN 诱导的肝损伤。[4]
本研究探讨了单侧注射 H1 受体拮抗剂氯苯那敏和 H2 受体拮抗剂雷尼替丁对基底神经节大细胞核 (NBM) 附近强化和焦虑参数的影响。在实验 1 中,将慢性植入导管的大鼠分别注射氯苯那敏或雷尼替丁(剂量分别为 0.1、1、10 和 20 μg),然后将其置于圆形开放场(封闭围栏)的四个限制象限之一中进行单次条件反射训练。在条件性围栏偏好测试中,只有注射了10或20 μg氯苯那敏的大鼠在四个象限中进行选择时,在处理过的围栏处停留的时间更长,表明氯苯那敏具有正强化作用。其他剂量的氯苯那敏或H2受体拮抗剂均未影响大鼠的偏好行为。在实验2中,我们使用高架十字迷宫(EPM)评估了基底膜内注射氯苯那敏或雷尼替丁(剂量分别为0.1、1、10和20 μg)的潜在抗焦虑或镇静作用。结果表明,单次注射0.1或20 μg氯苯那敏以及20 μg雷尼替丁在EPM中表现出相似的抗焦虑作用。两种化合物均增加了大鼠在开放臂上的停留时间,并增加了它们在开放臂边缘的扫描行为。其他剂量的H1和H2受体拮抗剂并未影响大鼠在EPM中的行为。总之,这些结果表明H1和H2受体拮抗剂对NBM中的强化和恐惧相关过程具有不同的调节作用,从而首次证明了该脑区的组胺能神经支配与行为相关。[5]
雷尼替丁曾是一种广泛用于治疗酸相关疾病的H2受体拮抗剂。它以多种剂型在药店和药房均有销售,包括Zantac。由于NDMA污染问题,该化合物于2019年在许多国家撤市。目前,雷尼替丁在大多数国家已不再作为药品销售。
*注: 文献方法仅供参考, InvivoChem并未独立验证这些方法的准确性
化学信息 & 存储运输条件
分子式
C13H22N4O3S.HCL
分子量
350.87
精确质量
314.141
元素分析
C, 49.66; H, 7.05; N, 17.82; O, 15.27; S, 10.20
CAS号
66357-35-5
相关CAS号
Ranitidine hydrochloride;66357-59-3
PubChem CID
3001055
外观&性状
Off-white to light brown solid at room temperature
密度
1.2±0.1 g/cm3
沸点
437.1±45.0 °C at 760 mmHg
熔点
69-70 °C ; MP: 133-134 °C /RATINIDINE HYDROCHLORIDE/
闪点
218.2±28.7 °C
蒸汽压
0.0±1.0 mmHg at 25°C
折射率
1.559
LogP
1.23
tPSA
111.56
氢键供体(HBD)数目
2
氢键受体(HBA)数目
7
可旋转键数目(RBC)
9
重原子数目
21
分子复杂度/Complexity
347
定义原子立体中心数目
0
SMILES
CNC(=C[N+](=O)[O-])NCCSCC1=CC=C(CN(C)C)O1
InChi Key
VMXUWOKSQNHOCA-UKTHLTGXSA-N
InChi Code
InChI=1S/C13H22N4O3S/c1-14-13(9-17(18)19)15-6-7-21-10-12-5-4-11(20-12)8-16(2)3/h4-5,9,14-15H,6-8,10H2,1-3H3/b13-9+
化学名
(E)-1-N'-[2-[[5-[(dimethylamino)methyl]furan-2-yl]methylsulfanyl]ethyl]-1-N-methyl-2-nitroethene-1,1-diamine
别名
ranitidine; 66357-35-5; Ranitidine Base; ranitidine hydrochloride; Raticina; Coralen; Gastrial; Quantor;
HS Tariff Code
2934.99.9001
存储方式

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

运输条件
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
溶解度数据
溶解度 (体外实验)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
溶解度 (体内实验)
注意: 如下所列的是一些常用的体内动物实验溶解配方,主要用于溶解难溶或不溶于水的产品(水溶度<1 mg/mL)。 建议您先取少量样品进行尝试,如该配方可行,再根据实验需求增加样品量。

注射用配方
(IP/IV/IM/SC等)
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO 50 μL Tween 80 850 μL Saline)
*生理盐水/Saline的制备:将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中,得到澄清溶液。
注射用配方 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (如: 100 μL DMSO 400 μL PEG300 50 μL Tween 80 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如: 100 μL DMSO 900 μL Corn oil)
示例: 注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液,加到 900 μL Corn oil/玉米油中, 混合均匀。
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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如:100 μL DMSO 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备(4°C,储存1周):将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中,得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如: 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精) 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如: 50 μL DMSO 100 μL PEG300 200 μL Castor oil 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (如: 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如: 100 μL EtOH 900 μL Corn oil)
注射用配方 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (如: 100 μL EtOH 400 μL PEG300 50 μL Tween 80 450 μL Saline)


口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中,得到0.5%CMC-Na澄清溶液;然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中,得到悬浮液。
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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合


注意: 以上为较为常见方法,仅供参考, InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型,对于某些尚未有文献报道溶解方法的化合物,需通过前期实验来确定(建议先取少量样品进行尝试),包括产品的溶解情况、梯度设置、动物的耐受性等。

请根据您的实验动物和给药方式选择适当的溶解配方/方案:
1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液));
2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方):
10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline);
假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL;

3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例;
4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶;
5、为保证最佳实验结果,工作液请现配现用!
6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们;
7、 以上所有助溶剂都可在 Invivochem.cn网站购买。
制备储备液 1 mg 5 mg 10 mg
1 mM 2.8501 mL 14.2503 mL 28.5006 mL
5 mM 0.5700 mL 2.8501 mL 5.7001 mL
10 mM 0.2850 mL 1.4250 mL 2.8501 mL

1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;

2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;

3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);

4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。

计算器

摩尔浓度计算器可计算特定溶液所需的质量、体积/浓度,具体如下:

  • 计算制备已知体积和浓度的溶液所需的化合物的质量
  • 计算将已知质量的化合物溶解到所需浓度所需的溶液体积
  • 计算特定体积中已知质量的化合物产生的溶液的浓度
使用摩尔浓度计算器计算摩尔浓度的示例如下所示:
假如化合物的分子量为350.26 g/mol,在5mL DMSO中制备10mM储备液所需的化合物的质量是多少?
  • 在分子量(MW)框中输入350.26
  • 在“浓度”框中输入10,然后选择正确的单位(mM)
  • 在“体积”框中输入5,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案17.513 mg出现在“质量”框中。以类似的方式,您可以计算体积和浓度。

稀释计算器可计算如何稀释已知浓度的储备液。例如,可以输入C1、C2和V2来计算V1,具体如下:

制备25毫升25μM溶液需要多少体积的10 mM储备溶液?
使用方程式C1V1=C2V2,其中C1=10mM,C2=25μM,V2=25 ml,V1未知:
  • 在C1框中输入10,然后选择正确的单位(mM)
  • 在C2框中输入25,然后选择正确的单位(μM)
  • 在V2框中输入25,然后选择正确的单位(mL)
  • 单击“计算”按钮
  • 答案62.5μL(0.1 ml)出现在V1框中
g/mol

分子量计算器可计算化合物的分子量 (摩尔质量)和元素组成,具体如下:

注:化学分子式大小写敏感:C12H18N3O4  c12h18n3o4
计算化合物摩尔质量(分子量)的说明:
  • 要计算化合物的分子量 (摩尔质量),请输入化学/分子式,然后单击“计算”按钮。
分子质量、分子量、摩尔质量和摩尔量的定义:
  • 分子质量(或分子量)是一种物质的一个分子的质量,用统一的原子质量单位(u)表示。(1u等于碳-12中一个原子质量的1/12)
  • 摩尔质量(摩尔重量)是一摩尔物质的质量,以g/mol表示。
/

配液计算器可计算将特定质量的产品配成特定浓度所需的溶剂体积 (配液体积)

  • 输入试剂的质量、所需的配液浓度以及正确的单位
  • 单击“计算”按钮
  • 答案显示在体积框中
动物体内实验配方计算器(澄清溶液)
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
第二步:请输入动物体内配方组成(配方适用于不溶/难溶于水的化合物),不同的产品和批次配方组成不同,如对配方有疑问,可先联系我们提供正确的体内实验配方。此外,请注意这只是一个配方计算器,而不是特定产品的确切配方。
+
+
+

计算结果:

工作液浓度 mg/mL;

DMSO母液配制方法 mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。

体内配方配制方法μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。

(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
            (2) 一定要按顺序加入溶剂 (助溶剂) 。

临床试验信息
Title:Flotetuzumab for the Treatment of Relapsed or Refractory Advanced CD123-Positive Hematological Malignancies
Status:Completed
updateDate:2026-01-28
Ctid:NCT04681105

Link: https://clinicaltrials.gov/ct2/show/NCT04681105

Conditions:Recurrent Acute Leukemia|Recurrent B Acute Lymphoblastic Leukemia|Recurrent Blastic Plasmacytoid Dendritic Cell Neoplasm|Recurrent Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Recurrent Hairy Cell Leukemia|Recurrent Hematologic Malignancy|Recurrent Hodgkin Lymphoma|Recurrent T Acute Lymphoblastic Leukemia|Refractory Acute Leukemia|Refractory B Acute Lymphoblastic Leukemia|Refractory Blastic Plasmacytoid Dendritic Cell Neoplasm|Refractory Chronic Myelogenous Leukemia, BCR-ABL1 Positive|Refractory Hairy Cell Leukemia|Refractory Hematologic Malignancy|Refractory Hodgkin Lymphoma|Refractory T Acute Lymphoblastic Leukemia|Systemic Mastocytosis
Interventions:Flotetuzumab
Phase:Phase 1
Title:A Study to Evaluate Efficacy, Safety, and Tolerability of Alemtuzumab in Pediatric Patients With RRMS With Disease Activity on Prior DMT
Status:Terminated
updateDate:2025-11-26
Ctid:NCT03368664

Link: https://clinicaltrials.gov/ct2/show/NCT03368664

Conditions:Multiple Sclerosis
Interventions:Other H1 antagonist
Phase:Phase 3
Title:Safely Stopping Pre-medications in Patients With Breast Cancer Who Are Receiving Paclitaxel
Status:Completed
updateDate:2025-08-20
Ctid:NCT04862585

Link: https://clinicaltrials.gov/ct2/show/NCT04862585

Conditions:Anatomic Stage 0 Breast Cancer AJCC v8|Anatomic Stage I Breast Cancer AJCC v8|Anatomic Stage IA Breast Cancer AJCC v8|Anatomic Stage IB Breast Cancer AJCC v8|Anatomic Stage II Breast Cancer AJCC v8|Anatomic Stage IIA Breast Cancer AJCC v8|Anatomic Stage IIB Breast Cancer AJCC v8|Anatomic Stage III Breast Cancer AJCC v8|Anatomic Stage IIIA Breast Cancer AJCC v8|Anatomic Stage IIIB Breast Cancer AJCC v8|Anatomic Stage IIIC Breast Cancer AJCC v8|Anatomic Stage IV Breast Cancer AJCC v8|Breast Carcinoma|Prognostic Stage 0 Breast Cancer AJCC v8|Prognostic Stage I Breast Cancer AJCC v8|Prognostic Stage IA Breast Cancer AJCC v8|Prognostic Stage IB Breast Cancer AJCC v8|Prognostic Stage II Breast Cancer AJCC v8|Prognostic Stage IIA Breast Cancer AJCC v8|Prognostic Stage IIB Breast Cancer AJCC v8|Prognostic Stage III Breast Cancer AJCC v8|Prognostic Stage IIIA Breast Cancer AJCC v8|Prognostic Stage IIIB Breast Cancer AJCC v8|Prognostic Stage IIIC Breast Cancer AJCC v8|Prognostic Stage IV Breast Cancer AJCC v8
Interventions:Ranitidine
Phase:Phase 2/Phase 3
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Status:Completed
updateDate:2024-10-30
Ctid:NCT05338502

Link: https://clinicaltrials.gov/ct2/show/NCT05338502

Conditions:Healthy
Interventions:Omeprazole
Phase:Phase 1
Title:Histamine Receptor 2 Antagonists as Enhancers of Anti-Tumour Immunity
Status:Completed
updateDate:2023-02-08
Ctid:NCT03145012

Link: https://clinicaltrials.gov/ct2/show/NCT03145012

Conditions:Cancer
Interventions:Ranitidine
Phase:Phase 4
Title:Rabeprazole Extended-Release 50 mg vs. Ranitidine 150 mg for Maintenance of Healed Erosive Gastroesophageal Reflux Disease (GERD)
Status:Completed
updateDate:2022-04-25
Ctid:NCT00838526

Link: https://clinicaltrials.gov/ct2/show/NCT00838526

Conditions:Gastroesophageal Reflux Disease (GERD)
Interventions:Ranitidine
Phase:Phase 3
Title:A Phase 2 Study of Isatuximab in Combination With Pomalidomide and Dexamethasone in MM Patients Who Received One Prior Line of Therapy Containing Lenalidomide and a Proteasome Inhibitor
Status:Unknown status
updateDate:2022-03-28
Ctid:NCT05298683

Link: https://clinicaltrials.gov/ct2/show/NCT05298683

Conditions:Multiple Myeloma|Renal Impairment|Neoplasms, Plasma Cell|Neoplasms by Histologic Type|Neoplasms|Paraproteinemias|Blood Protein Disorders|Hematologic Diseases
Interventions:Diphenhydramine (or equivalent)
Phase:Phase 2
Title:Safety and Efficacy of Isatuximab in Lymphoblastic Leukemia
Status:Terminated
updateDate:2022-03-21
Ctid:NCT02999633

Link: https://clinicaltrials.gov/ct2/show/NCT02999633

Conditions:T-cell Type Acute Leukemia-Precursor|T-lymphoblastic Lymphoma/Leukaemia
Interventions:diphenhydramine
Phase:Phase 2
Title:Clinical Study to Investigate the Urinary Excretion of N-nitrosodimethylamine (NDMA) After Ranitidine Administration
Status:Completed
updateDate:2021-08-09
Ctid:NCT04397445

Link: https://clinicaltrials.gov/ct2/show/NCT04397445

Conditions:Ranitidine Adverse Reaction|Pharmacokinetics|Food-drug Interaction
Interventions:Placebo
Phase:Phase 1
Title:Bronchial Hyper-responsiveness in Reflux Cough
Status:Terminated
updateDate:2019-07-23
Ctid:NCT00668317

Link: https://clinicaltrials.gov/ct2/show/NCT00668317

Conditions:Cough
Interventions:Ranitidine
Phase:Phase 3
Title:TPI 287 in Breast Cancer Metastatic to the Brain
Status:Completed
updateDate:2018-09-20
Ctid:NCT01332630

Link: https://clinicaltrials.gov/ct2/show/NCT01332630

Conditions:Breast Cancer
Interventions:Ranitidine
Phase:Phase 2
Title:A Crossover Study to Assess the Drug-drug Interaction of Acid Reducing Agent(s) on the Pharmacokinetics of a Single Oral Dose of Lumicitabine (JNJ-64041575) in Healthy Adult Participants
Status:Terminated
updateDate:2018-07-23
Ctid:NCT03468777

Link: https://clinicaltrials.gov/ct2/show/NCT03468777

Conditions:Healthy
Interventions:Ranitidine
Phase:Phase 1
Title:Nefopam vs Tramadol in the Prevention of Post Anaesthetic Shivering
Status:Unknown status
updateDate:2018-07-17
Ctid:NCT02441673

Link: https://clinicaltrials.gov/ct2/show/NCT02441673

Conditions:Post Anaesthetic Shivering
Interventions:oxytocin
Phase:Phase 2
Title:Ranitidin Versus Omeprazole in Patients Taking Clopidogrel
Status:Completed
updateDate:2018-07-06
Ctid:NCT01896557

Link: https://clinicaltrials.gov/ct2/show/NCT01896557

Conditions:Coronary Artery Disease|Drug Interaction Potentiation
Interventions:Clopidogrel
Phase:Phase 4
Title:Sublingual Misoprostol to Reduce Blood Loss During Elective Cesarean Delivery
Status:Unknown status
updateDate:2017-05-04
Ctid:NCT03140033

Link: https://clinicaltrials.gov/ct2/show/NCT03140033

Conditions:Hemorrhage Postpartum
Interventions:Ranitidine Oral Tablet
Phase:Phase 2
Title:Study in Healthy Volunteers to Assess Effect of Omeprazole and Ranitidine on the Pharmacokinetics of Vandetanib
Status:Completed
updateDate:2017-05-02
Ctid:NCT01539655

Link: https://clinicaltrials.gov/ct2/show/NCT01539655

Conditions:Medullary Thyroid Cancer
Interventions:ranitidine
Phase:Phase 1
Title:Pharmacokinetic Interaction Between Trospium With an Inhibitor of OCT1 and of P-gp in Subjects Genotyped for OCT1
Status:Completed
updateDate:2017-04-10
Ctid:NCT03011463

Link: https://clinicaltrials.gov/ct2/show/NCT03011463

Conditions:Pharmacokinetics|Inhibition Enzyme|Drug Interaction Potentiation
Interventions:oral administration of 500 mg clarithromycin
Phase:Phase 1
Title:Combination of Cabazitaxel With Prednisolone With Primary Prophylaxis With PEG-G-CSF in Treatment of Patients With Prostate Cancer
Status:Completed
updateDate:2017-01-24
Ctid:NCT02441894

Link: https://clinicaltrials.gov/ct2/show/NCT02441894

Conditions:Prostate Cancer
Interventions:Dexamethasone
Phase:Phase 4
Title:A Study to Evaluate The Effects of Two Different Meal Types, Omeprazole And Ranitidine On Danoprevir Pharmacokinetics When Coadministered With Ritonavir in Healthy Volunteers
Status:Completed
updateDate:2016-11-02
Ctid:NCT01392755

Link: https://clinicaltrials.gov/ct2/show/NCT01392755

Conditions:Healthy Volunteer
Interventions:ritonavir
Phase:Phase 1
Title:The Study of Eustachian Tube Dysfunction and Laryngopharyngeal Reflux
Status:Withdrawn
updateDate:2016-09-26
Ctid:NCT02123498

Link: https://clinicaltrials.gov/ct2/show/NCT02123498

Conditions:Eustachian Tube Dysfunction|Laryngopharyngeal Reflux
Interventions:Pantoprazole
Phase:Phase 4
Title:Management Of The Infusion-Associated Reactions In RRMS Patients Treated With LEMTRADA
Status:Completed
updateDate:2016-06-09
Ctid:NCT02205489

Link: https://clinicaltrials.gov/ct2/show/NCT02205489

Conditions:Relapsing-remitting Multiple Sclerosis
Interventions:paracetamol
Phase:Phase 4
Title:Does Pantoprazole Reduce the Anti-platelet Effect of Clopidogrel?
Status:Completed
updateDate:2016-04-11
Ctid:NCT02733640

Link: https://clinicaltrials.gov/ct2/show/NCT02733640

Conditions:Antiplatelet Effect
Interventions:Ranitidine
Phase:N/A
Title:Rabeprazole Extended Release 50 mg Versus Ranitidine 150 mg for Maintenance of Healed Erosive Gastroesophageal Reflux Disease (GERD)
Status:Completed
updateDate:2016-02-08
Ctid:NCT00839306

Link: https://clinicaltrials.gov/ct2/show/NCT00839306

Conditions:Gastroesophageal Reflux Disease (GERD)
Interventions:Ranitidine
Phase:Phase 3
Title:Proton Pump Inhibitors and Risk of Community-acquired Pneumonia
Status:Completed
updateDate:2015-09-22
Ctid:NCT02555852

Link: https://clinicaltrials.gov/ct2/show/NCT02555852

Conditions:Gastroesophageal Reflux Disease (GERD)|Community-acquired Pneumonia
Interventions:famotidine combinations
Phase:
Title:Comparison of Pantoprazole and Ranitidine in Dyspepsia
Status:Completed
updateDate:2015-07-23
Ctid:NCT01737840

Link: https://clinicaltrials.gov/ct2/show/NCT01737840

Conditions:Dyspepsia
Interventions:Ranitidine
Phase:Phase 4
Title:Comparison of Intravenous Omeprazole to Ranitidine on Recurrent Bleeding After Endoscopic Treatment of Bleeding Ulcer
Status:Withdrawn
updateDate:2015-04-03
Ctid:NCT00247130

Link: https://clinicaltrials.gov/ct2/show/NCT00247130

Conditions:Peptic Ulcers
Interventions:Ranitidine
Phase:Phase 4
Title:A Comparison of Efficacy of Intravenous Esomeprazole and Ranitidine Treatment of Dyspeptic Pain
Status:Completed
updateDate:2014-07-22
Ctid:NCT02197143

Link: https://clinicaltrials.gov/ct2/show/NCT02197143

Conditions:Dyspepsia
Interventions:hydrotalcid
Phase:Phase 4
Title:Tiotropium in Combination With Concomitant Cimetidine or Ranitidine in Healthy Male and Female Subjects
Status:Completed
updateDate:2014-06-24
Ctid:NCT02172417

Link: https://clinicaltrials.gov/ct2/show/NCT02172417

Conditions:Healthy
Interventions:Tiotropium
Phase:Phase 1
Title:Bioavailability of BIBR 953 ZW After Dose of BIBR 1048 MS
Status:Completed
updateDate:2014-06-23
Ctid:NCT02170792

Link: https://clinicaltrials.gov/ct2/show/NCT02170792

Conditions:Healthy
Interventions:Ranitidine
Phase:Phase 1
Title:Medical Treatment for Gastroesophageal Reflux Disease (GERD) in Preterm Infants
Status:Completed
updateDate:2014-01-15
Ctid:NCT00131248

Link: https://clinicaltrials.gov/ct2/show/NCT00131248

Conditions:Gastroesophageal Reflux
Interventions:placebo
Phase:Phase 3
Title:Lesinurad Interaction Study With Ranitidine
Status:Completed
updateDate:2014-01-09
Ctid:NCT01908257

Link: https://clinicaltrials.gov/ct2/show/NCT01908257

Conditions:Healthy
Interventions:lesinurad 400 mg + ranitidine 150 mg
Phase:Phase 1
Title:Effect of Ranitidine on Hyper-IgE Recurrent Infection (Job's) Syndrome
Status:Terminated
updateDate:2013-02-04
Ctid:NCT00527878

Link: https://clinicaltrials.gov/ct2/show/NCT00527878

Conditions:JOB's Syndrome|Hyper-IgE Recurrent Infection Syndrome|Immune Deficiency
Interventions:Placebo
Phase:Phase 2
Title:Extending Acute Stroke Trials to the Aerial Inter-hospital Transfer Setting
Status:Completed
updateDate:2013-01-16
Ctid:NCT00585351

Link: https://clinicaltrials.gov/ct2/show/NCT00585351

Conditions:Stroke
Interventions:Placebo
Phase:N/A
Title:Assess Pharmacokinetics of Fostamatinib in Fed and Fasted State in Combination With Ranitidine to Assess Bioavailability
Status:Completed
updateDate:2012-12-28
Ctid:NCT01682408

Link: https://clinicaltrials.gov/ct2/show/NCT01682408

Conditions:Pharmacokinetics
Interventions:Ranitidine
Phase:Phase 1
Title:BMS 247550 to Treat Kidney Cancer
Status:Completed
updateDate:2012-08-20
Ctid:NCT00030992

Link: https://clinicaltrials.gov/ct2/show/NCT00030992

Conditions:Renal Cell Carcinoma
Interventions:Diphenhydramine
Phase:Phase 2
Title:Effect of Single Doses of YF476 on Stomach Acidity Compared With Ranitidine and Placebo in Fasted and Fed States
Status:Completed
updateDate:2012-02-24
Ctid:NCT01538797

Link: https://clinicaltrials.gov/ct2/show/NCT01538797

Conditions:Reflux Oesophagitis
Interventions:Ranitidine
Phase:Phase 1
Title:A Comparative Efficacy and Safety Study of Nexium Delayed-Release Capsules (40mg qd and 20mg qd) Versus Ranitidine 150mg Bid for the Healing of NSAID-Associated Gastric Ulcers When Daily NSAID Use is Continued
Status:Completed
updateDate:2011-01-25
Ctid:NCT00633672

Link: https://clinicaltrials.gov/ct2/show/NCT00633672

Conditions:NSAID Associated Gastric Ulcers
Interventions:Esomeprazole
Phase:Phase 3
Title:Efficacy and Safety Study of Esomeprazole 20mg qd vs Ranitidine 150mg Bid in Patients With an NSAID-induced Gastric Ulcer
Status:Completed
updateDate:2010-07-08
Ctid:NCT00401752

Link: https://clinicaltrials.gov/ct2/show/NCT00401752

Conditions:Gastric Ulcer
Interventions:Ranitidine
Phase:Phase 3
Title:Bioequivalency Study of Ranitidine Tablets 300 mg of Dr. Reddy's Under Fasting Conditions
Status:Completed
updateDate:2010-06-09
Ctid:NCT01131702

Link: https://clinicaltrials.gov/ct2/show/NCT01131702

Conditions:Healthy
Interventions:Ranitidine
Phase:Phase 1
Title:A Comparative Efficacy and Safety Study of Nexium Delayed-Release Capsules (40mg qd and 20mg qd) Versus Ranitidine 150mg Bid for the Healing of NSAID-Associated Gastric Ulcers When Daily NSAID Use is Continued in Subjects in the US Only
Status:Completed
updateDate:2009-06-11
Ctid:NCT00633412

Link: https://clinicaltrials.gov/ct2/show/NCT00633412

Conditions:NSAID Associated Gastric Ulcers
Interventions:Esomeprazole
Phase:Phase 3
Title:A Clinico-Bacteriological Study and Effect of Stress Ulcer Prophylaxis on Occurrence of Ventilator Associated Pneumonia
Status:Completed
updateDate:2008-06-20
Ctid:NCT00702871

Link: https://clinicaltrials.gov/ct2/show/NCT00702871

Conditions:Ventilator Associated Pneumonia|Etiological Organisms|Antimicrobial Drug Susceptibility Pattern|Stress Ulcer Prophylaxis
Interventions:Sucralfate
Phase:Phase 4
Title:Gastric pH in Critically Ill Patients
Status:Completed
updateDate:2008-01-11
Ctid:NCT00590928

Link: https://clinicaltrials.gov/ct2/show/NCT00590928

Conditions:Critically Ill Patients|Indication for Stress Ulcer Prophylaxis
Interventions:ranitidine
Phase:Phase 4
Title:Comparison of a 'Step-Up' Versus a 'Step-Down' Treatment Strategy for Patients With New Onset Dyspepsia in General Practice (The DIAMOND-Study)
Status:Completed
updateDate:2007-08-29
Ctid:NCT00247715

Link: https://clinicaltrials.gov/ct2/show/NCT00247715

Conditions:Dyspepsia|Gastrointestinal Diseases
Interventions:pantoprazole
Phase:N/A
Title:Histamine Release and Implications of H1- and H2- Blockade in Adult Cardiac Surgery - A Randomised Controlled Study
Status:Prematurely Ended
Date:2005-04-27
Eudractnumber:2005-001291-12

Link: https://www.clinicaltrialsregister.eu/ctr-search/search?query=2005-001291-12

Condition:During cardiac surgery involving the use of cardiopulmonary bypass histamine is released in the blood. Histamine release has been related to an increased incidence of perioperative dysrhythmias and may be involved in other complications.Our aim is to find out whether the use of histamine blocking drugs will prevent these arrhythmias.The study population will consist of adult patients who must undergo elective cardiac surgery in which the use of cardiopulmonary bypass is necessary
Phase:Phase 4

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