Description
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.
Product information
CAS Number: 1366233-41-1
Molecular Weight: 411.88
Formula: C18H19ClFN3O3S
Chemical Name: 5-chloro-4-(2,3-dimethylpiperidine-1-carbonyl)-N-(6-fluoro-2H-1,3-benzodioxol-5-yl)-1,3-thiazol-2-amine
Smiles: CC1CCCN(C1C)C(=O)C1N=C(NC2C=C3OCOC3=CC=2F)SC=1Cl
InChiKey: GGKQWFQQUMWVOB-UHFFFAOYSA-N
InChi: InChI=1S/C18H19ClFN3O3S/c1-9-4-3-5-23(10(9)2)17(24)15-16(19)27-18(22-15)21-12-7-14-13(6-11(12)20)25-8-26-14/h6-7,9-10H,3-5,8H2,1-2H3,(H,21,22)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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). 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.
Products are for research use only. Not for human use.
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