Tropifexor

Lub npe tshuaj:

2-((1R,3r,5S)-3-((5-cyclopropyl-3-(2-(trifluoromethoxy)phenyl)isoxazol-4-yl)methoxy)-8-azabicyclo[3.2.1]octan-8- yl)-4-fluorobenzo[d]thiazole-6-carboxylic acid

SMILES Code:

FC(F)(F)OC(C=CC=C1)=C1C2=NOC(C3CC3)=C2CO[C@@H]4C[C@H]5N(C6=NC7=C(F)C=C( C(O)=O)C=C7S6)[C@H](CC5)C4

InChi Code:

InChI = 1S/C29H25F4N3O5S/c30-21-9-15(27(37)38)10-23-25(21)34-28(42-23)36-16-7-8-17(36)12- 18(11-16)39-13-20-24(NWS) 35-41-26(20)14-5-6-14)19-3-1-2-4-22(19)40-29(31,32)33/h1-4,9-10,14, 16-18H,5-8,11-13H2,(H,37,38)/t16-,17+,18+

InChi Key:

VYLOOGHLKSNNEK-PIIMJCKOSA-N

Lo lus tseem ceeb:

Tropifexor, LJN-452, LJN452, LJN 452, 1383816-29-2

Solubility:Soluble hauv DMSO

Cia:0 - 4 ° C rau lub sijhawm luv (hnub mus rau lub lis piam), lossis -20 ° C rau lub sijhawm ntev (hli).

Nqe lus piav qhia:

Tropifexor (compound 1) yog ib qho tshiab thiab muaj zog agonist ntawm FXR nrog EC50 ntawm 0.2 nM. Lub zog induction ntawm ob qho tib si BSEP thiab SHP cov noob yog pom nyob rau hauv thawj lub hlwb los ntawm Tropifexor nyob rau hauv ib tug concentration-dependent yam. BSEP induction saum lub tsheb (DMSO) tswj tau pom nyob rau hauv cov concentrations tsawg li 1 nM, thaum muaj zog induction ntawm SHP (15-fold saum lub tsheb) yog pom ntawm 10 nM thiab me me induction ntawm SHP ntawm 1 nM (3-fold)[1 ].

Hom phiaj: FXR