WS-12

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

WS-12 是一种有效的 TRPM8 激动剂，可作为清凉剂 (EC50：193 nM)。

WS-12 is a potent TRPM8 agonist that acts as a cooling agent (EC50 : 193 nM).

Acoltremon (10 μM) shows TRPM8 agonism in tests on heterologously expressed TRP ion channels.Acoltremon (1 or 10 μM; 0-250 s) shows highly potent and specific TRPM8 channel agonist in DRG neurons.Cell Viability Assay Cell Line:HEK293T cells Concentration:10 μM Incubation Time:Result:Activated mouse TRPM8 (mTRPM8), but neither activated nor inhibited mTRPA1.Cell Viability Assay Cell Line:Cultured mouse DRG neurons Concentration:1 or 10 μM Incubation Time:0-250 s Result:Showed approximately 10% to 14% of cultured wild-type neurons responsive to WS-12.

Acoltremon (intraperitoneal injection; 10 mg/kg; once) shows analgesic effect by selective TRPM8 activation in mice. Animal Model:Trpm8–/– mice and mice injected with Capsaicin Dosage:10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg; once Result:Produced an obvious analgesic effect, and this effect abolished in Trpm8–/– mice.Showed no change falling latencies in mice in the rotarod test.Reduced Capsaicin-induced nocifensive behavior.

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Membrane Transporter/Ion Channel

TRP/TRPV Channel

TRPM8

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68489-09-8

289.41

C18H27NO2

>98% (HPLC)

DMSO:20 mg/mL (69.11 mM)

COc1ccc(NC(=O)[C@@H]2C[C@H](C)CC[C@H]2C(C)C)cc1

(1R2S)-2-isopropyl-N-(4-methoxyphenyl)-5-methylcyclohexane-1-carboxamide

(-20℃)

With Ice Pack

≥ 2 years