GSK205 is a potent, selective TRPV4 antagonist with an IC50 of 4.19  μM for inhibiting TRPV4-mediated Ca2+ influx.

Product information

CAS Number: 1263068-83-2

Molecular Weight: 481.45

Formula: C24H25BrN4S

Chemical Name: N-(4-{2-[benzyl(methyl)amino]ethyl}phenyl)-5-(pyridin-3-yl)-1,3-thiazol-2-amine hydrobromide

Smiles: Br.CN(CC1C=CC=CC=1)CCC1C=CC(=CC=1)NC1=NC=C(S1)C1C=NC=CC=1

InChiKey: LQGOJHGNGSOUKL-UHFFFAOYSA-N

InChi: InChI=1S/C24H24N4S.BrH/c1-28(18-20-6-3-2-4-7-20)15-13-19-9-11-22(12-10-19)27-24-26-17-23(29-24)21-8-5-14-25-16-21;/h2-12,14,16-17H,13,15,18H2,1H3,(H,26,27);1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 250 mg/mL (519.26 mM; Need ultrasonic).

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:

GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist. GSK205 (5 μM; 4 days; T3-F442A adipocytes) treatment results in increases expression of thermogenic genes (Mcp1, Mip1α, Mcp3, Rantes and Vcam, et al.) and is also accompanied by a decrease in the proinflammatory gene program. This shift resembles the gene expression changes seen in TRPV4-deficient adipocytes.

In Vivo:

GSK205 (10 mg/kg; intraperitoneal injection; twice daily; for 7 days; for 4 weeks; male C57BL/6J mice) treatment shows significantly increases expression of thermogenic genes such as Ucp1, Pgc1a, Cidea and Cox8b. GSK205 treatment causes a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. GSK205 treatment significantly improves glucose tolerance in diet-induced obese (DIO) mice. There are no apparent sign of sickness or weight loss. GSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues.

Products are for research use only. Not for human use.