JNJ-39729209 | TRPV1 antagonist | Probechem Biochemicals

Chemical Structure : JNJ-39729209

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JNJ-39729209 (JNJ39729209)

货号: PC-63414Not For Human Use, Lab Use Only.

JNJ-39729209 is a potent, selective TRPV1 antagonist with binding pKi of 7.8 and 7.9 for human and rat TRPV1, respectively.

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生物&药学活性

JNJ-39729209 is a potent, selective TRPV1 antagonist with binding pKi of 7.8 and 7.9 for human and rat TRPV1, respectively.
JNJ-39729209 inhibits proton activation of human and rat TRPV1 receptors with pIC50s of 7.9 and 8.5, respectively, also prevents TRPV1 activation by capsaicin and heat.
JNJ-39729209 shows no agonist or antagonist activity forTRPV2, hTRPV4, or hTRPA1 at 10 uM.
JNJ-39729209 blocks capsaicin-induced hypotension, inducesa mild hyperthermia and inhibits capsaicin-induced hypothermia in vivo.
JNJ-39729209shows significant efficacy against carrageenan- and CFA-evoked thermal hyperalgesia and exhibits significant anti-tussive activity in a guinea-pig model of capsaicin-induced cough.

物理化学性质&存储条件

分子量	455.28
分子式	C19H11Cl2F3N4S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(2,6-dichlorobenzyl)-N-(4-(trifluoromethyl)phenyl)thiazolo[5,4-d]pyrimidin-7-amine

参考文献

1. Maher MP, et al. Eur J Pharmacol. 2011 Aug 1;663(1-3):40-50.

JNJ-39729209 (JNJ39729209)

生物&药学活性

物理化学性质&存储条件

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JNJ-39729209 (JNJ39729209)

生物&药学活性

物理化学性质&存储条件

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