GSK205 HBr

Product NameGSK205 HBr
CAS1263068-83-2
MFC24H25BrN4S
MW481.46
EINECS
MOL File1263068-83-2.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	DMSO: 250 mg/mL (519.26 mM)
form	Solid
color	Light yellow to yellow

Usage And Synthesis

Biological Activity

GSK205 is a potent and selective TRPV4 antagonist with IC50 of 4.19 μM, inhibits TRPV4-mediated Ca2+ influx.

in vitro

GSK205 HBr (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. < /p>

RT-PCR

Cell Line:	T3-F442A adipocytes
Concentration:	5 μM
Incubation Time:	4 days
Result:	Resulted in increased expression of thermogenic genes and is also accompanied by a decre ase in the proinflammatory gene program.

in vivo

GSK205 HBr (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 . It 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.
It has a relatively short half-life of 2 hours in the plasma and adipose tissues.

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Animal Model:	Male C57BL/ 6J mice with high-fat diet
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; twice daily; for 7 days < /td>
Result:	Caused a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat . Significantly improved glucose tolerance in diet-induced obese (DIO) mice.

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