DG172 dihydrochloride 是一种PPARβ/δ拮抗剂,IC50值为 27 nM。
产品描述
DG172 (dihydrochloride) is an antagonist of PPARβ/δ(IC50 : 27 nM).
体外活性
DG172 is a novel PPARβ/δ-selective ligand showing high binding affinity (IC(50) = 27 nM) and potent inverse agonistic properties.?DG172 selectively inhibited the agonist-induced activity of PPARβ/δ, enhanced transcriptional corepressor recruitment, and down-regulated transcription of the PPARβ/δ target gene Angptl4 in mouse myoblasts (IC(50) = 9.5 nM).?Importantly, DG172 was bioavailable after oral application to mice with peak plasma levels in the concentration range of its maximal inhibitory potency, suggesting that 37 will be an invaluable tool to elucidate the functions and therapeutic potential of PPARβ/δ[1].
Cas No.
1361504-77-9
分子式
C20H22BrCl2N3
分子量
455.22
别名
DG172 (dihydrochloride);DG-172 dihydrochloride;DG172 dihydrochloride
储存和溶解度
H2O:14.29 mg/mL (31.39 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years