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Apexbio Technology LLC RQ-00203078 1254205-52-1 10mg
Supplier: Apexbio Technology LLC B587210
RQ-00203078 (CAS 1254205-52-1) is a selective antagonist of the transient receptor potential melastatin 8 (TRPM8) ion channel a member of the TRP melastatin subfamily implicated in cold-induced pain hypersensitivity and neuropathic pain including chemotherapy-induced peripheral neuropathy diabetic neuropathy migraine and overactive bladder In in vitro assays RQ-00203078 inhibits menthol-induced TRPM8-mediated calcium influx with IC50 values of 8 3 nM in human and 5 8 nM in rat models demonstrating high selectivity over other TRP channels In vivo oral administration suppresses icilin-evoked tremors in rats in a dose-dependent manner (ED50 0 65 mg/kg) The compound remains in preclinical development and serves as a valuable tool for investigating TRPM8-related pathophysiology and potential therapeutic interventions
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