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SB-705498

产品编号 T6660Cas号 501951-42-4

SB705498 是一种口服有效的 TRPV1选择性拮抗剂,pIC50值为 7.1。

SB-705498
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SB-705498

纯度: ≥95%
产品编号 T6660Cas号 501951-42-4

SB705498 是一种口服有效的 TRPV1选择性拮抗剂,pIC50值为 7.1。

规格价格库存数量
1 mg¥ 151现货
5 mg¥ 397现货
10 mg¥ 738现货
25 mg¥ 1,530现货
50 mg¥ 2,390现货
100 mg¥ 3,400现货
200 mg¥ 4,720现货
1 mL x 10 mM (in DMSO)¥ 437现货
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产品介绍

生物活性
产品描述
SB705498 is a TRPV1 antagonist for hTRPV1. SB-705498 has been investigated for the treatment of Rhinitis, Chronic Cough, and Non-allergic Rhinitis.
靶点活性
TRPV1 (human):7.1(pIC50), TRPV1 (human):7.6(pKi)
体外活性
SB705498 (0.3 nM-1 μM) potently inhibits capsaicin-induced activation of human TRPV1 expressed in 1321N1 cells or HEK293 cells with apparent pKi of 7.5 or 7.6, respectively. Coapplication of 100 nM SB705498 rapidly, completely and reversibly inhibits hTRPV1 expressed in HEK293 cells. SB705498 has no significant effect on endogenous [Ca2+] responses in HEK293 cells produced by muscarinic acetylcholine receptor activation with carbachol or store-operated channel-mediated Ca2+ entry after depletion of intracellular stores with the Ca2+ pump inhibitor thapsigargin. SB705498 (10 pM-1 μM) also has no significant antagonist effect versus the close TRPV1 receptor paralog TRPV4 transiently expressed in HEK293 cells and activated using the synthetic ligand 4α-phorbol-12,13-didecanoate (10 μM). SB705498 reveals good antagonist potency against both the rat and guinea pig TRPV1. SB705498 antagonizes rat and guinea pig TRPV1 with pKi of 7.5 and 7.3, respectively. Coapplication of 100 nM to 10 μM SB705498 to the steady state of a maintained capsaicin response leads to rapid and complete inhibition of hTRPV1 at -70 mV. SB705498 inhibits capsaicin-mediated activation of hTRPV1 with IC50 of 3 nM and 17 nM at positive and negative holding potentials (-70 mV and + 70 mV), respectively. Coapplication of 1 μM SB705498 to the plateau period of the response produces complete and reversible inhibition of the TRPV1-mediated conductance. [1] SB705498 shows approximately equal activity versus multiple and diverse chemical and physical modes of TRPV1 receptor activation. SB705498 shows little or no activity versus a wide range of ion channels, receptors and enzymes. SB705498 produces full blockade of heat as well as pH activation of hTRPV1. [2]
体内活性
SB705498 exhibits potent and reversible blockade against the multiple modes of TRPV1 activation, namely the vanilloid (capsaicin), heat- and acid-mediated activation of the receptor. SB705498 displays excellent activity at 10 and 30 mg/kg po with good reversal of allodynia. SB705498 is also shown to give 80% reversal of allodynia in the guinea pig FCA model at 10 mg/kg p.o. [2]
化学信息
分子量429.23
分子式C17H16BrF3N4O
CAS No.501951-42-4
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
Ethanol: 16 mg/mL (37.3 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 60 mg/mL (139.79 mM)
溶液配制表
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.3298 mL11.6488 mL23.2975 mL116.4877 mL
5 mM0.4660 mL2.3298 mL4.6595 mL23.2975 mL
10 mM0.2330 mL1.1649 mL2.3298 mL11.6488 mL
20 mM0.1165 mL0.5824 mL1.1649 mL5.8244 mL
DMSO
1mg5mg10mg50mg
50 mM0.0466 mL0.2330 mL0.4660 mL2.3298 mL
100 mM0.0233 mL0.1165 mL0.2330 mL1.1649 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:
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。
% DMSO
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%ddH2O

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