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Ranitidine

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Rating icon 很棒

纯度: 99.52%

货号 T3610Cas号 66357-35-5

别名 雷尼替丁, Ranitidin, HSDB 3925

Ranitidine (HSDB 3925) 是一种选择性的,具有口服活性的组胺 H2 受体拮抗剂,IC50为 3.3 μM。它还一种是CYP2C19和CYP2C9的弱抑制剂,可抑制胃液分泌。

Ranitidine

Ranitidine

一键复制产品信息
Rating icon 很棒

纯度: 99.52%

货号 T3610 别名 雷尼替丁, Ranitidin, HSDB 3925Cas号 66357-35-5

Ranitidine (HSDB 3925) 是一种选择性的,具有口服活性的组胺 H2 受体拮抗剂,IC50为 3.3 μM。它还一种是CYP2C19和CYP2C9的弱抑制剂,可抑制胃液分泌。

规格价格库存数量
5 mg
¥ 266
现货
10 mg
¥ 379
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25 mg
¥ 659
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50 mg
¥ 968
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100 mg
¥ 1,430
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200 mg
¥ 2,130
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500 mg
¥ 3,450
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1 mL x 10 mM (in DMSO)
¥ 323
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纯度: 99.52%
颜色: 红色
性状: Viscous
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产品介绍


Ranitidine AI Summary
Ranitidine exhibits significant histamine H2 and H3 receptor antagonistic activities with KB values of 6.3E-8 and 0.0000012, respectively, indicating its high potency in inhibiting these receptors. The compound demonstrates a binding affinity to the histamine H2 receptor with a pKB value of 7.2 and shows an inhibitory effect on histamine-induced responses in animal models, including a 72% inhibition of gastric acid secretion in rats and a 44% inhibition of chronotropic response in guinea pig right atrium. It also inhibits acetylcholinesterase with an IC50 of 650 nM and enhances gastrointestinal motility with an EC30 of 1.8 µM in guinea pig ileum. Pharmacokinetic studies reveal that Ranitidine has a volume of distribution (Vdss) of 1.3 L.kg-1, a high fraction unbound in plasma (Fu = 0.85), and a pKa of 8.47, suggesting good distribution within the body. The compound is moderately absorbed in the human GI tract (50% absorption) and displays low intrinsic clearance in human hepatocytes, suggesting metabolic stability. Despite its pronounced pharmacological activities, Ranitidine exhibits low permeability across biological membranes, with permeability values ranging from 0.2 to 5.6 x 10^-6 cm/s in various assays, and is characterized by low lipophilicity (logD7.4 = -0.29). It also possesses hepatic clearance with a logCL value of 0.4624 and weak inhibition activity against several transporters and enzymes, implying limited potential for significant metabolic interactions. Additionally, the compound has shown some degree of liver toxicity, reflected in changes in liver enzyme levels. Overall, Ranitidine presents as a potent histamine receptor antagonist with sizable effects on gastrointestinal and enzymatic activities, coupled with pharmacokinetic properties that favour distribution and stability but are limited by low permeability and moderate-to-high potential for hepatotoxicity..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Ranitidine (HSDB 3925) is a non-imidazole blocker of those histamine receptors that mediate gastric secretion (H2 receptors). It is used to treat gastrointestinal ulcers.
靶点活性
H2 receptor:3.3 μM (IC50)
别名雷尼替丁, Ranitidin, HSDB 3925
化学信息
分子量314.40
分子式C13H22N4O3S
CAS No.66357-35-5
SmilesC(N(C)C)C=1OC(CSCCNC(=CN(=O)=O)NC)=CC1
密度1.184 g/cm3
储存&溶解度
存储Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
溶解度信息
DMSO: 250 mg/mL (795.17 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween-80+45% Saline: 2.5 mg/mL (7.95 mM), Sonication is recommended.
请按顺序添加溶剂,在添加下一种溶剂之前,尽可能使溶液澄清。如有必要,可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考,体内配方并不是绝对的,请根据不同情况进行调整。
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.1807 mL15.9033 mL31.8066 mL159.0331 mL
5 mM0.6361 mL3.1807 mL6.3613 mL31.8066 mL
10 mM0.3181 mL1.5903 mL3.1807 mL15.9033 mL
20 mM0.1590 mL0.7952 mL1.5903 mL7.9517 mL
50 mM0.0636 mL0.3181 mL0.6361 mL3.1807 mL
100 mM0.0318 mL0.1590 mL0.3181 mL1.5903 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 混匀澄清
以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。
方案所需的各类助溶剂如: DMSOPEG300PEG400Tween 80SBE-β-CD玉米油等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

剂量转换

对于不同动物的给药剂量换算,您也可以参考 更多

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