TRPC3/6-IN-1

Names

[ CAS No. ]:
736945-96-3

[ Name ]:
TRPC3/6-IN-1

Biological Activity

[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]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel
Research Areas >> Cardiovascular Disease

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C20H19N3O2S

[ Molecular Weight ]:
365.45

Related Compounds