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Tolbutamide sodium

别名: TOLBUTAMIDE SODIUM; Tolbutamide sodium salt; 473-41-6; Sodium tolbutamide; Orinase Diagnostic; Sodium butamide; Sodium orinase; Tolbutamide sodium, sterile; 甲苯磺丁脲;丁脲;甲磺丁脲;苯磺丁脲
目录号: V41310 纯度: ≥98%
COA 产品数据 产品说明书 SDS
甲苯磺丁脲钠（也称为 HLS 831；商品名：Artosin、Diabetol、Orinase）是一种有效的选择性钾通道抑制剂，最初用作口服降血糖药物。
Tolbutamide sodium CAS号: 473-41-6
产品类别: New1
产品仅用于科学研究，不针对患者销售
规格 价格
500mg
1g
Other Sizes
大包装询价
020-31522723 sales@invivochem.cn

Other Forms of Tolbutamide sodium:

  • Tolbutamide-13C (Tolbutamide 13C)
  • 4-Hydroxytolbutamide-d9 (Hydroxytolbutamide-d9)
  • Tolbutamide-d9 (甲苯磺丁脲 d9)
  • 甲苯磺丁脲
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InvivoChem产品被CNS等顶刊论文引用
产品描述
甲苯磺丁脲钠（也称为 HLS 831；商品名：Artosin、Diabetol、Orinase）是一种有效的选择性钾通道抑制剂，最初用作口服降血糖药物。该药物可用于治疗 II 型糖尿病。据报道，Tolbutamide 可抑制基础和环 AMP 刺激的蛋白激酶活性，环 AMP 依赖性激酶活性的 IC50 值为 4mM。此外，Tolbutamide 可抑制犬心脏的可溶性蛋白激酶和膜结合蛋白激酶。
生物活性&实验参考方法
靶点
K/potassium channel; CYP2C9; antidiabetic
体外研究 (In Vitro)
体外活性：甲苯磺丁脲属于一类称为磺酰脲类的药物。甲苯磺丁脲通过使胰腺产生胰岛素（一种分解体内糖所需的天然物质）并帮助身体有效利用胰岛素来降低血糖。这种药物只能帮助身体自然产生胰岛素的人降低血糖。甲苯磺丁脲不用于治疗 1 型糖尿病（身体不产生胰岛素，因此无法控制血液中的糖含量）或糖尿病酮症酸中毒（如果不治疗高血糖，可能会出现的严重病症） ）。 Tolbutamide 抑制基础和环 AMP 刺激的蛋白激酶活性，Tolbutamide 的 IC50 为 4 mM。对于由激素（去甲肾上腺素和 ACTH）或二丁酰环 AMP 加茶碱诱导的体外脂肪分解的半最大抑制，需要类似的甲苯磺丁脲浓度。甲苯磺丁脲还抑制犬心脏的可溶性和膜结合蛋白激酶。甲苯磺丁脲对脂肪组织环 AMP 依赖性蛋白激酶的抑制是该药物抗脂肪分解作用的一种可能解释。 Tolbutamide 通过增加 Cx43 抑制 C6 神经胶质瘤细胞增殖，这与 Cdk 抑制剂 p21 和 p27 上调导致的 pRb 磷酸化减少相关。胞质核苷酸通过对抑制性和刺激性受体的联合作用，增强小鼠胰腺 B 细胞中 ATP 依赖性 K+ 通道对甲苯磺丁脲的敏感性。激酶测定：断头后获得喂养的 Wistar 大鼠（175-225 gm）的切块附睾脂肪垫，并在含有 1.27 mM CaCl2 的 Krebs-碳酸氢盐缓冲液中于 37°C 孵育两小时。添加后，甲苯磺丁脲仅在孵育期间存在。孵育后，在冷的克雷布斯碳酸氢盐缓冲液中冲洗脂肪垫并进行超声处理。在 4 °C 下以 50,000 × g 离心 30 分钟所得的水性上清液每毫升含有 0.75 至 1.25 毫克蛋白质，并测定了环 AMP 刺激的蛋白激酶活性。该测定在 0.2 mL 中进行，添加了 10 μmol 甘油磷酸钠 pH 7.0、2 μmol 氟化钠、0.4 μmol 茶碱、0.1 μmol 乙二醇双（β-氨基乙基醚）-N, N-四乙酸、3 μmol 氯化镁、0.3 mg 混合组蛋白、2 nmole (γ- 32P) ATP、1 nmole 环 AMP（指定时）和 0.05 ml 上清液。细胞测定：每次实验前，将 C6 神经胶质瘤细胞在无血清 DMEM 中于 37°C 孵育至少 24 小时。甲苯磺丁脲 (400 μM) 在无血清培养基中孵育 24 小时。孵化在 37 °C、95% 空气/5% CO2、90–95% 湿度的气氛中进行。
体内研究 (In Vivo)
450 mg Tolbutamide/kg/天，连续 7 天显着增加胰岛素与分离脂肪细胞的结合。结合曲线反映了受体位点数量的增加而不是亲和力的增加。这种效应与脂肪组织对胰岛素的反应增强有关，因为与对照组相比，用甲苯磺丁脲处理的动物的脂肪细胞在胰岛素存在下将更多的葡萄糖转化为脂质。然而，只有在大剂量甲苯磺丁脲时才能观察到胰岛素结合位点的增加，这降低了胰腺胰岛素含量、离体胰腺的分泌反应和血清胰岛素水平。较小的剂量足以通过刺激胰岛素分泌产生代谢作用，但不会提供额外的胰岛素结合位点
细胞实验
在目前的研究中，研究人员表明，甲磺丁脲和dbcAMP增加了肿瘤抑制蛋白Cx43的合成，并降低了Ki-67的水平，Ki-67是细胞增殖时表达的一种蛋白质。这些效应伴随着pRb磷酸化的减少，主要是在Ser-795上，Ser-795是控制细胞增殖的关键残基。pRb磷酸化的减少不太可能是由D型细胞周期蛋白水平的降低介导的，因为用甲磺丁脲或dbcAMP治疗后，D1和D3的表达略有增加，而不是减少细胞周期蛋白的表达。然而，经甲磺丁脲和dbcAMP处理后，Cdk抑制剂p21和p27上调，表明它们可能参与了pRb磷酸化的减少。当Cx43被siRNA沉默时，根据Ki-67表达判断，甲磺丁脲和dbcAMP都不能上调p21，从而减少胶质瘤细胞增殖。总之，甲磺丁脲和dbcAMP通过增加Cx43抑制C6胶质瘤细胞增殖，这与Cdk抑制剂p21和p27上调导致的pRb磷酸化减少有关[2]。
动物实验
The functional state of beta cells may influence the rate of their destruction in Type 1 (insulin-dependent) diabetes mellitus. We examined the effect of diazoxide, which inhibits insulin secretion, or tolbutamide, which stimulates insulin secretion, upon the incidence of diabetes in the non-obese-diabetic (NOD) mouse. Female mice were treated from 3-30 weeks of age with diet containing diazoxide 250 mg.kg-1 or tolbutamide 125 mg.kg-1. The cumulative incidence of diabetes at 35 weeks was similar in the diazoxide (16 of 24) and control (18 of 24) groups, but reduced in the tolbutamide group (10 of 23, p < 0.04 vs control group). In a second experiment, treatment was started from 9 weeks of age, by which time insulitis is already present. The cumulative incidence of diabetes at 35 weeks was 16 of 24 in controls, 15 of 24 on diazoxide and 11 of 24 on tolbutamide (p = NS vs control). A third experiment compared the effect of treatment from 3 weeks with control diet or diet containing tolbutamide 125 mg.kg-1 or 500 mg.kg-1. Diabetes was reduced by tolbutamide treatment, with a cumulative incidence of 25 of 31 in controls, 18 of 30 on tolbutamide 125 mg.kg-1 (p < 0.04) and 14 of 32 on 500 mg.kg-1 (p < 0.002), although the difference between the two treatment groups failed to reach statistical significance. A fourth experiment showed that treatment from 3-12 weeks with diazoxide 1000 mg.kg-1 increased the extent of insulitis compared with controls and animals treated with tolbutamide 500 mg.kg-1.[3]
Pretreatment of pregnant BALB/c mice with several low doses of tolbutamide protected against the fetolethal effects of a high dose. Pregnant mice were given single ip injections of 400 mg/kg in saline on day 13; 100 mg/kg/day on days 10, 11, 12, and 13; or 100 mg/kg/day on days 10, 11, and 12 and 400 mg/kg on day 13. On day 16 the single-treatment group had a significantly higher resorption rate than any other group. Fetolethality was not related to hypoglycemia. The protective effect of pretreatment may have been due to induction of maternal microsomal enzymes.[4]
药代性质 (ADME/PK)
Absorption
Readily absorbed following oral administration. Tolbutamide is detectable in plasma 30-60 minutes following oral administration of a single dose with peak plasma concentrations occurring within 3-5 hours. Absorption is unaltered if taken with food but is increased with high pH.
Route of Elimination
Unchanged drug and metabolites are eliminated in the urine and feces. Approximately 75-85% of a single orally administered dose is excreted in the urine principally as the 1-butyl-3-p-carboxyphenylsulfonylurea within 24 hours.

AFTER ORAL ADMIN, SULFONYLUREAS ARE RAPIDLY ABSORBED. /SULFONYLUREAS/

TOLBUTAMIDE CAN BE DETECTED IN BLOOD WITHIN 30 MIN AFTER ORAL ADMIN; PEAK CONCN ARE REACHED WITHIN 3 TO 5 HR. .../IT/ IS BOUND TO PLASMA PROTEINS. ... HALF-LIFE OF TOLBUTAMIDE IS ABOUT 5 HR.

IN CONTRAST TO STUDIES REPORTED IN ANIMALS, METABOLIC CLEARANCE OF...TOLBUTAMIDE IN MAN HAS BEEN SHOWN TO BE UNALTERED BY FASTING.

Excreted (percentage)...100
Metabolism / Metabolites Metabolized in the liver principally via oxidation of the p-methyl group producing the carboxyl metabolite, 1-butyl-3-p-carboxyphenylsulfonylurea. May also be metabolized to hydroxytolbutamide. Tolbutamide does not undergo acetylation like antibacterial sulfonamides as it does not have a p-amino group.

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...MAJOR TOLBUTAMIDE METAB IN MAN HAS BEEN IDENTIFIED AS 1-BUTYL-3-P-CARBOXYPHENYLSULFONYLUREA... 1-BUTYL-3-P-HYDROXYMETHYLPHENYLSULFONYLUREA IS ALSO FORMED IN SMALL AMT.

IN RAT, MAJOR URINARY METAB, 1-BUTYL-3-P-HYDROXYMETHYLPHENYLSULFONYLUREA COMPRISED 75% OF DOSE, BUT SMALL AMT OF 1-BUTYL-3-P-CARBOXYPHENYLSULFONYLUREA & P-TOLYLSULFONYLUREA, COMPRISING 5% OF DOSE, WERE ALSO PRESENT.

ALTHOUGH 1-BUTYL-3-P-HYDROXYMETHYLPHENYLSULFONYLUREA HAS BEEN REPORTED AS PRINCIPAL METAB IN CAT.../IT IS CLAIMED/ THAT CAT METABOLIZES TOLBUTAMIDE IN SAME WAY AS DOG. .../IT HAS BEEN SHOWN/ THAT TOLBUTAMIDE IS TRANSFORMED INTO 1-BUTYL-3-P-CARBOXYPHENYLSULFONYLUREA IN GUINEA PIGS & RABBITS.

IN CONTRAST TO RATS, RABBITS & MAN, DOGS METABOLIZE TOLBUTAMIDE...INTO P-TOLYLSULFONYLUREA & P-TOLYLSULFONAMIDE BY MECHANISM INVOLVING HYDROLYSIS.

Tolbutamide has known human metabolites that include 4-Hydroxytolbutamide.

Biological Half-Life
Approximately 7 hours with interindividual variations ranging from 4-25 hours. Tolbutamide has the shortest duration of action, 6-12 hours, of the antidiabetic sulfonylureas.

Half-life...3-25 /hours/

毒性/毒理 (Toxicokinetics/TK)
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Tolbutamide is no longer marketed in the United States. It is excreted into breastmilk in small amounts that should cause no harm to the breastfed infant. Monitor breastfed infants for signs of hypoglycemia such as jitteriness, excessive sleepiness, poor feeding, seizures cyanosis, apnea, or hypothermia. If there is concern, monitoring of the breastfed infant's blood glucose is advisable during maternal therapy with hypoglycemic agents.

◉ Effects in Breastfed Infants
Relevant published information was not found as of the revision date.

◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
Interactions
SULFAPHENAZOLE ENHANCES ACTION OF TOLBUTAMIDE & MAY CAUSE SYMPTOMS OF SEVERE HYPOGLYCEMIA IN DIABETIC PT. IT IS UNCLEAR WHETHER THIS INTERACTION ALSO OCCURS WITH OTHER SULFONAMIDES OR SULFONYLUREA COMPD.

HYPOGLYCEMIC ACTIVITY OF TOLBUTAMIDE MAY BE ENHANCED BY CONCURRENT ADMIN OF PHENYLBUTAZONE, & DOWNWARD ADJUSTMENT OF TOLBUTAMIDE DOSAGE MAY BE INDICATED. ... ALTHOUGH NOT DOCUMENTED, OXYPHENBUTAZONE & POSSIBLY SULFINPYRAZONE CAN BE EXPECTED TO INTERACT SIMILARLY TO PHENYLBUTAZONE.

SINCE MAO INHIBITORS MAY ENHANCE HYPOGLYCEMIC ACTION OF INSULIN IN ANIMALS & IN HUMAN DIABETIC PT, CONCURRENT ADMIN OF MAO INHIBITORS & INSULIN TO DIABETIC SUBJECTS MAY BE POTENTIALLY DANGEROUS. .../TOLBUTAMIDE HAS/ BEEN REPORTED TO INTERACT WITH MAO INHIBITORS.
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National Toxicology Program Studies
A bioassay of tolbutamide for possible carcinogenicity was conducted by admin the test material in the diet to Fischer 344 rats and B6C3F1 mice. Groups of 35 rats of each sex were admin tolbutamide at one of two doses, either 12,000 or 24,000 ppm, 5 days/wk for 78 wk, then observed for an additional 28 wk. Matched control groups consisted of 15 untreated rats of each sex. All surviving rats were /sacrificed/ at 102-104 wk. Groups of 35 mice of each sex were admin tolbutamide at one of two doses, either 25,000 or 50,000 ppm, 5 days/wk for 78 wk, then observed for an additional 24-26 wk. Matched control groups consisted of 15 untreated mice of each sex. All surviving mice were /sacrificed/ at 102-104 wk. Mean body weights of the treated rats and mice were lower than those of the corresponding matched controls during the entire study; however, survival was not significantly affected by treatment in either species. In both sexes of both species, survival was considered to be adequate for meaningful statistical analyses of the incidence of tumors. In both the rats and mice, a variety of neoplasms were found in both the tolbutamide treated and control groups. None of the neoplasms were present in statistically significant incr incidence in treated groups of either species as compared with control groups and were not considered to be cmpd related. It is concluded that under the conditions of this bioassay, tolbutamide was not carcinogenic for either Fischer 344 rats or B6C3F1 mice. Levels of Evidence of Carcinogenicity: Male Rats: Negative; Female Rats: Negative; Male Mice: Negative; Female Mice: Negative.

Protein Binding
Approximately 95% bound to plasma proteins.

参考文献

[1]. Opposite effects of tolbutamide and diazoxide on the ATP-dependent K+ channel in mouse pancreatic beta-cells. Pflugers Arch. 1986 Nov;407(5):493-9.

[2]. Glucose and tolbutamide induce apoptosis in pancreatic beta-cells. A process dependent on intracellular Ca2+ concentration. J Biol Chem. 1998 Dec 11;273(50):33501-7.
其他信息
Tolbutamide Sodium is the sodium salt form of tolbutamide, a short-acting, first-generation sulfonylurea with hypoglycemic activity. Compared to second-generation sulfonylureas, tolbutamide is more likely to cause adverse effects, such as jaundice. This agent is rapidly metabolized by CYPC29.
See also: Tolbutamide (has active moiety).
*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
C12H17N2O3S-.NA+
分子量
292.32978
精确质量
270.104
CAS号
473-41-6
相关CAS号
Tolbutamide;64-77-7;Tolbutamide-d9;1219794-57-6
PubChem CID
23690448
外观&性状
Typically exists as solid at room temperature
密度
1.184g/cm3
折射率
1.532
LogP
3.459
tPSA
87.14
氢键供体(HBD)数目
1
氢键受体(HBA)数目
4
可旋转键数目(RBC)
5
重原子数目
19
分子复杂度/Complexity
360
定义原子立体中心数目
0
SMILES
[Na+].CCCCNC([N-]S(C1C=CC(C)=CC=1)(=O)=O)=O
InChi Key
QKHDBRQBSNZFAK-UHFFFAOYSA-M
InChi Code
InChI=1S/C12H18N2O3S.Na/c1-3-4-9-13-12(15)14-18(16,17)11-7-5-10(2)6-8-11;/h5-8H,3-4,9H2,1-2H3,(H2,13,14,15);/q;+1/p-1
化学名
sodium;butylcarbamoyl-(4-methylphenyl)sulfonylazanide
别名
TOLBUTAMIDE SODIUM; Tolbutamide sodium salt; 473-41-6; Sodium tolbutamide; Orinase Diagnostic; Sodium butamide; Sodium orinase; Tolbutamide sodium, sterile;
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 : PEG300 ：Tween 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: 以注射用配方 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 : PEG300：Tween 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: 以口服配方 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 3.4208 mL 17.1040 mL 34.2079 mL
5 mM 0.6842 mL 3.4208 mL 6.8416 mL
10 mM 0.3421 mL 1.7104 mL 3.4208 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
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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。
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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
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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。
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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。
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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：取 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
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05097716 Completed
Has Results		 Drug: Ritlecitinib
Drug: Tolbutamide		 Healthy Volunteers Pfizer November 2, 2021 Phase 1
NCT01185548 Terminated
Has Results		 Drug: Tolbutamide
Drug: Tasisulam		 Lymphoma
Advanced Cancer		 Eli Lilly and Company July 2010 Phase 1
NCT03291288 Completed
Has Results		 Drug: Tolbutamide
Drug: Midazolam		 Drug Interaction Potential Daiichi Sankyo February 26, 2018 Phase 1
NCT03716427 Completed Drug: CT1812
Drug: tolbutamide		 Healthy Volunteers Cognition Therapeutics November 10, 2016 Phase 1
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