I-Tropifexor

Igama Lekhemikhali:

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

Ikhodi ye-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

Ikhodi ye-InChi:

I-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+

I-InChi Key:

VYLOOGHLKSNNEK-PIIMJCKOSA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga).

Incazelo:

I-Tropifexor (inhlanganisela 1) iyinoveli futhi i-agonist enamandla kakhulu ye-FXR ene-EC50 ye-0.2 nM. Ukufakwa okuqinile kokubili kofuzo lwe-BSEP ne-SHP kubonakala kumaseli ayinhloko yi-Tropifexor ngendlela encike ekugxilweni. Ukufakwa kwe-BSEP ngenhla kokulawulwa kwemoto (DMSO) kubonwa ekugxiliseni okuphansi njenge-1 nM, kuyilapho ukufakwa okuqinile kwe-SHP (i-15-fold ngenhla kwemoto) kubonwa ku-10 nM kanye nokungeniswa okuncane kwe-SHP ku-1 nM (3-fold) [1 ].

Ithagethi: FXR