Tropifexor

Inoa Kimia:

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

Code 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+

Ki InChi:

VYLOOGHLKSNNEK-PIIMJCKOSA-N

huaʻōlelo:

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

Hiki ke hoʻoheheʻe:Hiki ke hoʻoheheʻe ʻia ma DMSO

Waihona:0 - 4°C no ka wā pōkole (nā lā i nā pule), a i ʻole -20°C no ka wā lōʻihi (mau mahina).

wehewehe:

ʻO Tropifexor (compound 1) kahi moʻolelo a me ka agonist ikaika loa o FXR me kahi EC50 o 0.2 nM. ʻIke ʻia ka induction ikaika o nā genes BSEP a me SHP i loko o nā keena mua e Tropifexor ma kahi ʻano hilinaʻi. ʻIke ʻia ka BSEP induction ma luna o ka kaʻa (DMSO) ma nā ʻano haʻahaʻa haʻahaʻa e like me 1 nM, aʻo ka hoʻokomo ikaika ʻana o SHP (15-fold ma luna o ka kaʻa) e nānā ʻia ma 10 nM a me ka hoʻokomo haʻahaʻa o SHP ma 1 nM (3-fold) [1 ].

Kuhikuhi: FXR