Cilofexor (GS-9674) 是一种有效的、选择性的、具有口服活性的非甾体 FXR 激动剂,EC50 为 43 nM。
Cas No. | 1418274-28-8 |
别名 | GS-9674 |
化学名 | 2-[3-[2-chloro-4-[[5-cyclopropyl-3-(2,6-dichlorophenyl)-4-isoxazolyl]methoxy]phenyl]-3-hydroxy-1-azetidinyl]-4-pyridinecarboxylic acid |
Canonical SMILES | OC(C1=CC=NC(N2CC(C3=C(Cl)C=C(OCC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)C=C3)(O)C2)=C1)=O |
分子式 | C28H22Cl3N3O5 |
分子量 | 586.9 |
溶解度 | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:5): 0.16 mg/ml,DMSO: 15 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Cilofexor inhibits binding of a synthetic peptide, comprising residues 676-700 of the steroid receptor coactivator 1 (SRC-1), to the farnesoid X receptor (FXR; EC50 =<25 nm in a fret activity assay). it has fxr agonist mammalian one hybrid (m1h) assay (ec50 =>100 nM). |