GSK2332255B 

GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC₅₀s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels^[1].

Nuclear factor of activated T cells (NFAT) activation by Ang II ( angiotensin II) is blocked in a dose dependent manner by GSK255B (0.01, 0.1, and 1 μM) in HEK293T cells overexpressing TRPC3. GSK255B blocks NFAT activation by Ang II in HEK293T cells expressing a mutant TRPC6 channel with T70 and S322 mutated to glutamic acid (SETE)^[1].
GSK255B (10 μM) blocks calcium entry stimulated by Phenylephrine (20 μM) in rat neonatal cardiac myocytes. GSK255B dose-dependent blockade of cell hypertrophy signaling triggered by angiotensin II or endothelin-1 in HEK293T cells as well as in neonatal and adult cardiac myocytes^[1].

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

411.88

C₁₈H₁₉ClFN₃O₃S

1366233-41-1

O=C(C1=C(Cl)SC(NC2=C(F)C=C(OCO3)C3=C2)=N1)N4C(C)C(C)CCC4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Kinya Seo, et al. Combined TRPC3 and TRPC6 blockade by selective small-molecule or genetic deletion inhibits pathological cardiac hypertrophy. Proc Natl Acad Sci U S A. 2014 Jan 28;111(4):1551-6.  [Content Brief]