736945-96-3

736945-96-3 structure
736945-96-3 structure
  • Name: TRPC3/6-IN-1
  • Chemical Name: TRPC3/6-IN-1
  • CAS Number: 736945-96-3
  • Molecular Formula: C20H19N3O2S
  • Molecular Weight: 365.45
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
  • Create Date: 2022-09-12 23:09:35
  • Modify Date: 2024-04-06 19:46:59
  • TRPC3/6-IN-1 is a potent selectivity and orally active molecule blocker of the canonical transient receptor channels (TRPC3/6), has block potency for hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. TRPC3/6-IN-1 can be used for the research of chronic models of heart failure[1].

Name TRPC3/6-IN-1
Description TRPC3/6-IN-1 is a potent selectivity and orally active molecule blocker of the canonical transient receptor channels (TRPC3/6), has block potency for hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively. TRPC3/6-IN-1 can be used for the research of chronic models of heart failure[1].
Related Catalog
Target

hTRPC3:1260 nM (IC50)

hTRPC6:500 nM (IC50)

In Vitro TRPC3/6-IN-1 has block potency for hTRPC3 and hTRPC6 with IC50 values of 1260 nM and 500 nM, respectively[1].
In Vivo TRPC3/6-IN-1 has good blocking activity for TRPC3 and TRPC6 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
References

[1]. David G Washburn, et al. The discovery of potent blockers of the canonical transient receptor channels, TRPC3 and TRPC6, based on an anilino-thiazole pharmacophore. Bioorg Med Chem Lett. 2013 Sep 1;23(17):4979-84.

Molecular Formula C20H19N3O2S
Molecular Weight 365.45