TRPV1 antagonist 3

• CAT Number: I043891
• CAS Number: 2765294-54-8
• Purity: ≥95%
• Synonyms: (2S)-2-(5-phenyl-1,3-thiazol-2-yl)-N-(3-propan-2-ylphenyl)pyrrolidine-1-carboxamide
• InChI: InChI=1S/C23H25N3OS/c1-16(2)18-10-6-11-19(14-18)25-23(27)26-13-7-12-20(26)22-24-15-21(28-22)17-8-4-3-5-9-17/h3-6,8-11,14-16,20H,7,12-13H2,1-2H3,(H,25,27)/t20-/m0/s1
• InChIKey: CZISSZWUQQBGMU-FQEVSTJZSA-N
• SMILES: CC(C)C1=CC(=CC=C1)NC(=O)N2CCCC2C3=NC=C(S3)C4=CC=CC=C4

TRPV1 antagonist 3 (Compound 7q) is a potent TRPV1 antagonist with an IC50 of 2.66 nM against capsaicin. TRPV1 antagonist 3 is mode-selective, oral bioavailable (F = 60%) and CNS-penetrant[1].
TRPV1 antagonist 3 (Compound 7q) is highly selective for the TRPV1 receptor relative to other TRP channels[1].
TRPV1 antagonist 3 shows acceptable aqueous solubility (solubility at pH 7.4 = 26 μg/mL) [1].
TRPV1 antagonist 3 (Compound 7q) (0-30 mg/kg; i.p.; 30 min) shows anti-nociceptive effect mainly mediated by blocking CAP-activated channel[1].
TRPV1 antagonist 3 (0-100 mg/kg; i.g.) had no obvious thermal effect in rats[1].
TRPV1 antagonist 3 (10 mg/kg; i.v.) shows a good concentration in the brain at 0.5 h, with value of 2311 ng/g, and has good CNS penetration, with a brain/plasma ratio of 1.66[1].