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CAS No. : 1254205-52-1
MCE 国际站:RQ-00203078
产品活性:RQ-00203078 是一种高选择性,有效且具有口服活性的 TRPM8 拮抗剂,对大鼠和人类 TRPM8 通道的 IC50 分别为 5.3 nM 和 8.3 nM。RQ-00203078 对 TRPV1,TRPA1,TRPV4 或 TRPM2 通道几乎没有抑制作用。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:TRP Channel
In Vitro: Intracellular Ca2+ imaging reveals that menthol induced both intracellular Ca2+ release and store-operated Ca2+ entry, with RQ-00203078 inhibiting each effect. RQ-00203078 (1-10 μM) inhibits HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.
In Vivo: RQ-00203078 (compound 36) demonstrates excellent in vivo activity in a dose dependent manner with an ED50 value of 0.65 mg/kg in the Icilin-induced wet-dog shakes model in rats after oral administration.
Excellent oral exposure of RQ-00203078 (compound 36) is confirmed independently in rat pharmacokinetics studies at 3 mg/kg (p.o.) administration, with a Cmax value of 2300 ng/mL and 86% bioavailability.
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