半岛bd体育手机客户端 说明

一般描述

A cell-permeable and orally available pyridylsulfone compound that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC₅₀in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 ?M against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in culturesin vitro(IC₅₀= 126 nM against 2 nM GW501516-induced reporter transcription in CV-1 cells) and in micein vivo(82% and 71% inhibition of 10 mg/kg GW0742-inducedAdrpandAngptl4mRNA upregulation, respectively, in colon epithelium by 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys²⁴⁹. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 ?M GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 ?M GW1929 in the presence or absence of 1 ?M GSK3787, respectively).
A cell-permeable pyridylsulfone that acts as a selective, high affinity PPARβ (PPARδ) ligand (IC₅₀in PPAR ligand displacement assays = 200 nM against human PPARβ and >10 ?M against PPARα or PPARγ) and effectively antagonizes agonist-induced, but not basal, PPARβ transcription activity both in culturesin vitro(IC₅₀= 126 nM in CV-1 cells) and in micein vivo(82% and 71% inhibition of 10 mg/kg GW0742-inducedAdrpandAngptl4mRNA upregulation, respectively, in colon epithelium; 10 mg/kg GSK3787; p.o.) by covalently modifying PPARβ at Cys²⁴⁹. GSK3787 is also shown to exhibit weak agonistic activity toward PPARγ (1.2-fold increase above basal level by 1 ?M GSK3787), and effectively block the more potent agonist GW1929 (Cat. Nos. 370695) from further stimulation (1.5 and 3.5-fold above basal by 0.3 ?M GW1929 in the presence or absence of 1 ?M GSK3787, respectively).

包装

10 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Palkar, P.S., et al. 2010.Mol. Pharmacol.78,419.
Shearer, B,G., et al. 2010.J. Med. Chem.53,1857.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

半岛bd体育手机客户端 性质

安全信息