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A 784168
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产品介绍
产品介绍
产品信息
纯化方式
>99%
抗原名称
TRPV1 channel
来源纯化
Synthetic
商品描述
CHEMBL482834;A Potent Blocker of TRPV1 Channel;A 784168 (#A-345) is a highly pure, synthetic, and biologically active compound.
分子量
479.4
生物活性
A 784168 is a potent TRPV1 antagonist, inhibiting human TRPV1 activation by 50 nM capsaicin with IC50 of 25 nM1.
纯度
>99%
可溶性
100 mM in DMSO or 50 mM in ethanol. Centrifuge all product preparations before use (10000 x g 5 min).
浓度
10 nM - 1 µM.
形式
Lyophilized
背景
别名
1-[3-(trifluoromethyl)pyridin-2-yl]-N-[4-(trifluoromethylsulfonyl)phenyl]-3,6-dihydro-2H-pyridine-4-carboxamide.
背景
A 784168 is a synthetic and potent antagonist of the TRPV1 channel. A 784168 inhibits human TRPV1 activation by 50 nM capsaicin with an IC50 of 25 nM. A 784168 was found to produce inhibition in 1321N1 astrocytoma cells expressing recombinant human TRPV1 and also in HEK 293 cells. In addition to its inhibition of TRPV1, A 784168 was found to be a very weak antagonist of TRPM8 (IC50 = 20.8 µM) with no effect on TRPA1 channels and a variety of receptors including adenosine, angiotensin, α- and β-adrenergic receptors. A 784168 has a plasma binding capacity of 93.5±0.9% and oral bioavailability of 33%. A 784168 volume of distribution is 12.4L/kg and it has high blood-brain barrier penetrance. Administration of oral A 784168 reduces acute nociceptive behavior induced by capsaicin injection and chronic thermal hyperalgesia induced by CFA injection in a rat model1.
分子式
C19H15F6N3O3S.
CAS号
824982-41-4
制备和贮存
存储溶液
Up to four weeks at 4°C or three months at -20°C.
保存方式
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.;Up to four weeks at 4°C or three months at -20°C.
数据库链接
pubmed id
11420211
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