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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-TRP Channel-PF-05105679
PF-05105679

Chemical Structure : PF-05105679

CAS No.: 1398583-31-7

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PF-05105679 (PF 05105679;PF05105679)

货号: PC-60785Not For Human Use, Lab Use Only.

PF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition).

规格 价格 库存 数量
5 mg ￥1180 In stock
10 mg ￥1880 In stock
25 mg ￥3280 In stock
50 mg ￥5480 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

PF-05105679 is a potent, selective TRPM8 channel inhibitor with IC50 of 103 nM (human TRPM8 currents inhibition).
PF-05105679 displays >100-fold selectivity against a broad panel of 90 receptors, ion channels, and enzymes.
PF-05105679 demonstrates moderately potency against agonist (WS-12) and cold modalities of activation of TRPM8 in plate-based assay formats with IC50 of 181 and 480 nM, respectively, shows increased potency on voltage activation in HEK-293 cells at 12°C with IC50 of 13.8 nM.
PF-05105679 demonstrates activity in vivo in the guinea pig bladder ice water and menthol challenge tests with an IC50 of 200 nM and reduces core body temperature in the rats, and reduces pain in the cold pressor test in humans.

物理化学性质&存储条件

分子量 428.463
分子式 C26H21FN2O3
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

(R)-3-[(1-(4-fluorophenyl)ethyl)(quinolin-3-ylcarbonyl)amino]methylbenzoic acid

参考文献

1. Winchester WJ, et al. J Pharmacol Exp Ther. 2014 Nov;351(2):259-69.

2. Andrews MD, et al. ACS Med Chem Lett. 2015 Jan 30;6(4):419-24.

3. Gosset JR, et al. Eur J Pharm Sci. 2017 Nov 15;109S:S161-S167.

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