Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GSK205 is a selective TRPV4 antagonist (IC50: 4.19 μM) for inhibiting TRPV4-mediated Ca2+ influx.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 6-8 weeks | $ 766.00 | |
50 mg | 6-8 weeks | $ 996.00 | |
100 mg | 6-8 weeks | $ 1,740.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 250 mg/mL (519.26 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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GSK205 1263068-83-2 Others GSK 205 GSK-205 inhibitor inhibit