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Product Name | RQ-00203078 |
Description | Purity >98%. RQ-00203078 is a selective antagonist of transient receptor potential melastatin 8 (TRPM8; IC50 s = 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). It attenuates icilin-induced wet-dog shakes in rats (ED50 = 0.65 mg/kg) after oral administration. RQ-00203078 has been shown to reduce HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro . 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. |
Size | n/a |
Concentration | n/a |
Applications | n/a |
Other Names | 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-benzoic acid |
Gene, Accession, CAS # | CAS: 1254205-52-1 |
Catalog # | LS-H9774 |
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Order / More Info | RQ-00203078 from LIFESPAN BIOSCIENCES INC. |
Product Specific References | n/a |
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