RQ-00203078

RQ-00203078

CAT N°: 19075
Price:

48.00 40.80

RQ-00203078 is a selective antagonist of transient receptor potential melastatin 8 (TRPM8; IC50s = 8.3 and 5.8 nM in human and rat, respectively), while having little inhibitory action against TRPV1 (IC50 > 30 µM), TRPA1 (IC50 > 10 µM), TRPV4 (IC50 = 10 µM), or TRPM2 channels (IC50 > 10 µM).{31190} It attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg) after oral administration.{31190} RQ-00203078 has been shown to reduce HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.{31191} TRPM8, a member of the TRP melastatin subgroup, plays a role in cold hyperalgesia and cold allodynia caused by disease conditions such as chemotherapy-induced peripheral neuropathy, diabetic neuropathy, migraine, and overactive bladder. It is also known to be involved in the tumor progression of certain carcinomas.

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