TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist ( IC50 = 33.06 nM), moderate to weak URAT1 ( IC50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. TRPV1 antagonist 10 has analgesic and urate-lowering effect. TRPV1 antagonist 10 can be studied for research in hyperuricemia and inflammatory pain [1].
In Vivo, TRPV1 antagonist 10 (Compound 39) (3-20 mg/kg, p.o., one single dose) shows dose-dependent analgesic effect in both Formalin-induced phase I and phase II pain in male Kunming mice model[1]. TRPV1 antagonist 10 (10-20 mg/kg, p.o., 21 consecutive days) reduces the uric acid level and improves the renal function at 20 mg/kg in hyperuricemia mice model[1]. TRPV1 antagonist 10 (500 mg/kg, p.o., one single dose) leads to no obvious abnormal behaviors and difference in weight and food intake in healthy Kunming mice[1]. TRPV1 antagonist 10 (100 mg/kg, p.o., every other day for 14 consecutive days) leads to no obvious abnormal behaviors and difference in weight and food intake in healthy Kunming mice[1].
In Vitro, TRPV1 antagonist 10 (Compound 39) (50 μM, 24 h) shows 60.25% inhibition rate against GLUT9 in UA (1 mM)-treated HEK293T cells[1]. TRPV1 antagonist 10 (0-400 μM, 24-72 h) exhibits higher levels of cytotoxicity on HepG2 and HK2 cells with increasing dose and time of incubation[1]. TRPV1 antagonist 10 (0-100 μM, 3-20 min) shows high metabolic stability in human and rat liver microsomes[1].
References:
[1]. Chunxia Liu, et al., Structure Optimization of Natural Product Piperine to Obtain Novel and Potent Analogs with Anti-inflammation Pain and Urate-Lowering Effect, European Journal of Medicinal Chemistry, 2025, 117649, ISSN 0223-5234
In Vivo, TRPV1 antagonist 10 (Compound 39) (3-20 mg/kg, p.o., one single dose) shows dose-dependent analgesic effect in both Formalin-induced phase I and phase II pain in male Kunming mice model[1]. TRPV1 antagonist 10 (10-20 mg/kg, p.o., 21 consecutive days) reduces the uric acid level and improves the renal function at 20 mg/kg in hyperuricemia mice model[1]. TRPV1 antagonist 10 (500 mg/kg, p.o., one single dose) leads to no obvious abnormal behaviors and difference in weight and food intake in healthy Kunming mice[1]. TRPV1 antagonist 10 (100 mg/kg, p.o., every other day for 14 consecutive days) leads to no obvious abnormal behaviors and difference in weight and food intake in healthy Kunming mice[1].
In Vitro, TRPV1 antagonist 10 (Compound 39) (50 μM, 24 h) shows 60.25% inhibition rate against GLUT9 in UA (1 mM)-treated HEK293T cells[1]. TRPV1 antagonist 10 (0-400 μM, 24-72 h) exhibits higher levels of cytotoxicity on HepG2 and HK2 cells with increasing dose and time of incubation[1]. TRPV1 antagonist 10 (0-100 μM, 3-20 min) shows high metabolic stability in human and rat liver microsomes[1].
References:
[1]. Chunxia Liu, et al., Structure Optimization of Natural Product Piperine to Obtain Novel and Potent Analogs with Anti-inflammation Pain and Urate-Lowering Effect, European Journal of Medicinal Chemistry, 2025, 117649, ISSN 0223-5234