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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-JNJ-17203212
JNJ-17203212

Chemical Structure : JNJ-17203212

CAS No.: 821768-06-3

JNJ-17203212 (JNJ17203212;JNJ 17203212)

货号: PC-42062Not For Human Use, Lab Use Only.

JNJ-17203212 is a potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.

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5 mg ¥780 In stock
10 mg ¥1180 In stock
25 mg ¥2180 In stock
50 mg ¥3680 In stock
100 mg Get quote

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

JNJ-17203212 is a potent, selective and orally bioavailable TRPV1 receptor antagonist with IC50 of 65 nM and 102 nM for hTRPV1 and rTRPV1, respectively.
JNJ-17203212 exhibits high selectivity against a panel of receptors and transporters, and does not inhibits related TRP channels TRPV2, TRPV4, or TRPA1.
JNJ-17203212 inhibits both pH (pIC50=7.23) and capsaicin (pIC50=6.32)-induced channel activation.
JNJ-17203212 attenuates capsaicin evoked coughs, prevents core hypothermia evoked by capsaicin in vivo.

物理化学性质&存储条件

分子量 419.3243
分子式 C17H15F6N5O
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

1-Piperazinecarboxamide, 4-[3-(trifluoromethyl)-2-pyridinyl]-N-[5-(trifluoromethyl)-2-pyridinyl]-

参考文献

1. Swanson DM, et al. J Med Chem. 2005 Mar 24;48(6):1857-72.

2. Bhattacharya A, et al. J Pharmacol Exp Ther. 2007 Nov;323(2):665-74.

3. Cefalu JS, et al. J Urol. 2009 Aug;182(2):776-85.

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