| 规格 | 价格 | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| 靶点 |
5-HT3 Receptor
|
|---|---|
| 体外研究 (In Vitro) |
雷莫司琼 (1 μM) 抑制豚鼠结肠粘膜中 5-HT3 受体依赖性 5-HT 释放 [3]。
|
| 体内研究 (In Vivo) |
雷莫司琼(0.01-0.1 mg/kg,口服,每天两次,连续 5 天)可减轻 C57BL/6 小鼠 5-氟尿嘧啶 (5-FU) 诱发的肠粘膜炎 [2]。
|
| 参考文献 | |
| 其他信息 |
拉莫司琼属于吲哚类药物。
拉莫司琼是一种5-羟色胺3型(5-HT3)受体拮抗剂,常用于治疗恶心、呕吐以及某些腹泻疾病。据信,其效力高于其他第一代5-HT3受体拮抗剂(例如昂丹司琼),且止吐作用更持久。目前,拉莫司琼仅在日本和部分东南亚国家获准使用。 拉莫司琼是一种选择性5-羟色胺(5-HT)受体拮抗剂,具有潜在的止吐活性。给药后,拉莫司琼选择性地与位于迷走神经末梢和中枢神经系统(CNS)呕吐中枢的5-HT3受体结合并阻断其活性,从而抑制化疗引起的恶心和呕吐。 另见:盐酸昂丹司琼(相关药物)。盐酸拉莫司琼(活性部分)。 药物适应症 用于治疗男性恶心呕吐和腹泻为主的肠易激综合征。 |
| 分子式 |
C17H17N3O
|
|---|---|
| 分子量 |
279.34
|
| 精确质量 |
279.137
|
| CAS号 |
132036-88-5
|
| PubChem CID |
108000
|
| 外观&性状 |
Typically exists as solids at room temperature
|
| 密度 |
1.3±0.1 g/cm3
|
| 沸点 |
579.7±50.0 °C at 760 mmHg
|
| 闪点 |
304.4±30.1 °C
|
| 蒸汽压 |
0.0±1.6 mmHg at 25°C
|
| 折射率 |
1.708
|
| LogP |
1.99
|
| tPSA |
50.68
|
| 氢键供体(HBD)数目 |
1
|
| 氢键受体(HBA)数目 |
2
|
| 可旋转键数目(RBC) |
2
|
| 重原子数目 |
21
|
| 分子复杂度/Complexity |
413
|
| 定义原子立体中心数目 |
1
|
| SMILES |
CN1C2C(=CC=CC=2)C(C(C2CC3NC=NC=3CC2)=O)=C1
|
| InChi Key |
NTHPAPBPFQJABD-LLVKDONJSA-N
|
| InChi Code |
InChI=1S/C17H17N3O/c1-20-9-13(12-4-2-3-5-16(12)20)17(21)11-6-7-14-15(8-11)19-10-18-14/h2-5,9-11H,6-8H2,1H3,(H,18,19)/t11-/m1/s1
|
| 化学名 |
(1-methylindol-3-yl)-[(5R)-4,5,6,7-tetrahydro-3H-benzimidazol-5-yl]methanone
|
| 别名 |
YM060 free base
|
| 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 (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
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *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。 View More
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)] 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。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 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 | 3.5799 mL | 17.8993 mL | 35.7987 mL | |
| 5 mM | 0.7160 mL | 3.5799 mL | 7.1597 mL | |
| 10 mM | 0.3580 mL | 1.7899 mL | 3.5799 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) 。
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