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GSK205

Catalog No. T11480   CAS 1263068-83-2

GSK205 is a selective TRPV4 antagonist (IC50: 4.19 μM) for inhibiting TRPV4-mediated Ca2+ influx.

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GSK205 Chemical Structure
GSK205, CAS 1263068-83-2
Pack Size Availability Price/USD Quantity
1 mg 5 days $ 64.00
50 mg 6-8 weeks $ 996.00
100 mg 6-8 weeks $ 1,740.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description GSK205 is a selective TRPV4 antagonist (IC50: 4.19 μM) for inhibiting TRPV4-mediated Ca2+ influx.
Targets&IC50 TRPV4:4.19  μM
In vitro 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.GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist.
In vivo 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.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.
Molecular Weight 481.45
Formula C24H25BrN4S
CAS No. 1263068-83-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 250 mg/mL (519.26 mM), Need ultrasonic

( < 1 mg/ml refers to the product slightly soluble or insoluble )

TargetMolReferences and Literature

1. Ye L, et al. TRPV4 is a regulator of adipose oxidative metabolism, inflammation, and energy homeostasis. Cell. 2012 Sep 28;151(1):96-110. 2. Kanju P, et al. Small molecule dual-inhibitors of TRPV4 and TRPA1 for attenuation of inflammation and pain. Sci Rep. 2016 Jun 1;6:26894.

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Keywords

GSK205 1263068-83-2 Others GSK 205 GSK-205 inhibitor inhibit

 

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