M353-0039

M353-0039 (50 seconds) potently and selectively inhibits UT-A2 in human UT-A2-overexpressing HEK293F cells with an IC₅₀ of 0.35 μM, showing no activity against UT-A3 or UT-B^[1].
M353-0039 (10-100 μM; 30 minutes) does not inhibit rat UT-A1-mediated urea transport in stably expressing MDCK cells^[1].
M353-0039 (10 nM-100 μM; 6 minutes) does not inhibit mouse UT-B-mediated urea transport in erythrocytes^[1].
M353-0039 (10 μM; 5 minutes) inhibits urea transport in human HepG2 cells, confirming UT-A2-mediated urea efflux in these hepatic cells^[1].
M353-0039 (50 μM) binds deeply to UT-A2, forming more interactions than prior inhibitors, including critical contacts in the unique "T-T" subpocket, which underpins its superior inhibitory potency^[1].
M353-0039 (50 seconds) demonstrates that the C285 residue in UT-A2 is critical for its binding and inhibitory activity, as mutating it to alanine reduces potency and mutating it to tryptophan abolishes activity^[1].
M353-0039 (100 μM; 24 hours) exhibits no cytotoxicity toward MDCK cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.