RQ-00203078

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). 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.Formal Name: 4-[[[3-chloro-5-(trifluoromethyl)-2-pyridinyl][[4-(trifluoromethoxy)phenyl]methyl]amino]sulfonyl]-benzoic acid. CAS Number: 1254205-52-1. Molecular Formula: C21H13ClF6N2O5S. Formula Weight: 554.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml, DMSO: 25 mg/ml, Ethanol: 25 mg/ml. lambdamax: 234, 278 nm. SMILES: OC(C1=CC=C(S(N(CC2=CC=C(OC(F)(F)F)C=C2)C3=NC=C(C(F)(F)F)C=C3Cl)(=O)=O)C=C1)=O. InChi Code: InChI=1S/C21H13ClF6N2O5S/c22-17-9-14(20(23,24)25)10-29-18(17)30(11-12-1-5-15(6-2-12)35-21(26,27)28)36(33,34)16-7-3-13(4-8-16)19(31)32/h1-10H,11H2,(H,31,32). InChi Key: IJGQFZYYEHCCIZ-UHFFFAOYSA-N.