Description
GSK417651A (736945-96-3) is a TRPC blocker. In whole-cell patch-clamp experiments in HEK293 cells transfected with recombinant human TRPC3 or TRPC6, GSK417651A blocked both TRPC3 and TRPC6 current with IC50 of ~0.04 μM.1?Combined pharmacological blockade of TRPC3 and TRPC6 inhibits cardiac hypertrophy.2 Cell permeable
Uses
GSK417651A is an inhibitor of transient receptor channels 3 & 6.
in vivo
TRPC3/6-IN-1 (compound 3) has good pharmacokinetic in rats[1].
Pharmacokinetic Parameters of TRPC3/6-IN-1 in rats [1].
| Compd | Dose(iv)(mg/kg) | Cmax(iv)(ng/ml) | CL(iv)(ml/min/kg) | MRT(iv)(h) | DNAUC(iv)(h?kg/L) | %F |
| 3 | 0.93 | 250 | 120 | 0.3 | 0.14 | ~1 |
IC 50
hTRPC3: 1260 nM (IC50); hTRPC6: 500 nM (IC50)
References
1) Xu et al. (2013), Characterization of small molecule TRPC3 and TRPC6 agonists and antagonists; Biophys. J., 104 Supp 1 454a
2) Seo et al. (2014) Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy; Proc. Natl. Acad. Sci. USA, 111 1551
