Tropifexor

Ingoa matū:

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

Waehere SMILES:

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

Waehere InChi:

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(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+

Kī InChi:

VYLOOGHLKSNNEK-PIIMJCKOSA-N

Kupumatua:

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

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama).

Whakaahuatanga:

Ko te Tropifexor (compound 1) he pukapuka me te agonist tino kaha o FXR me te EC50 o 0.2 nM. Ko te whakauru pakari o nga ira BSEP me te SHP ka kitea i roto i nga pūtau tuatahi e Tropifexor i runga i te kukū-whakaaro. Ko te whakaurunga BSEP i runga ake i te waka (DMSO) ka kitea i nga kohinga iti iho i te 1 nM, i te wa e kitea ana te whakauru kaha o te SHP (15-fold i runga ake i te waka) i te 10 nM me te whakauru ngawari o te SHP i te 1 nM (3-fold) [1 ].

Whāinga: FXR