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ReN-1869 hydrochloride

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产品编号 T12703Cas号 170149-76-5
别名 NNC-05-1869 hydrochloride

ReN 1869 hydrochloride is a novel, selective antagonist of histamine H1 receptor.

ReN-1869 hydrochloride

ReN-1869 hydrochloride

Rating icon 还可以
产品编号 T12703 别名 NNC-05-1869 hydrochlorideCas号 170149-76-5

ReN 1869 hydrochloride is a novel, selective antagonist of histamine H1 receptor.

规格价格库存数量
25 mg¥ 10,6006-8周
50 mg¥ 13,8006-8周
100 mg¥ 17,5006-8周
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产品介绍

生物活性
产品描述
ReN 1869 hydrochloride is a novel, selective antagonist of histamine H1 receptor.
靶点活性
H1 receptor:ki:0.19±0.04 μM
体外活性
ReN 1869 is a highly selective tricyclic antihistamine that shows functional histamine H1 receptor antagonism.?ReN 1869 is profiled for activity at 10 μM at various receptors, transporters, enzymes and ion channels.?ReN 1869 only demonstrates affinity to the histamine H1 receptor (guinea pig brain, [3H]pyrilamine) with a Ki of 0.19±0.04 μM and the non-selective σ site [guinea pig brain, [3H]1,3-di-tolylguanidine (DTG)] with a Ki of 0.45 μM.?ReN 1869 dose-dependently reduces the responses with IC50 of 1.70±0.002 μM.
体内活性
ReN 1869 is a novel, selective histamine H(1) receptor antagonist.?It is orally available, well tolerated, easily enters the central nervous system (CNS) but no adverse effects are seen in mice at 300 mg/kg.?ReN 1869 at 0.01-10 mg/kg is antinociceptive in tests of chemical nociception in rodents (formalin, capsaicin, phenyl quinone writhing) but not in thermal tests (hot plate and tail flick).?ReN 1869 amplifies the analgesic action of morphine but does not show tolerance after chronic dosing.?Moreover, the compound is effective against inflammation of neurogenic origin (antidromic nerve stimulation, histamine-evoked edema) but not in carrageenan-induced inflammation.?We suggest that ReN 1869, via H(1) blockade, counteracts the effect of histamine liberated from activated mast cells and inhibits pain transmission in the dorsal spinal cord.?ReN 1869 represents a new class of antihistamines with pain-relieving properties that probably is mediated centrally through histamine H(1) receptors but alternative mechanisms of action cannot be excluded.
别名NNC-05-1869 hydrochloride
化学信息
分子量397.94
分子式C24H28ClNO2
CAS No.170149-76-5
密度no data available
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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:
TargetMol | Animal experiments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 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% 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 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 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:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 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。

1 请输入动物实验的基本信息
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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。
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