Ọgwụgwọ nke Tropifexor

Aha kemịkalụ:

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

Koodu Ọchịchọ:

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

Koodu 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+

Igodo InChi:

VYLOOGHLKSNNEK-PIIMJCKOSA-N

Okwu:

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

Solubility:Soluble na DMSO

Nchekwa:0 - 4 Celsius C maka obere oge (ụbọchị ruo izu), ma ọ bụ -20 Celsius maka ogologo oge (ọnwa).

Nkọwa:

Tropifexor (mkpokọta 1) bụ akwụkwọ akụkọ na nnukwu ike agonist nke FXR nwere EC50 nke 0.2 nM. A na-ahụ ntinye siri ike nke mkpụrụ ndụ BSEP na SHP na mkpụrụ ndụ ndị mbụ site na Tropifexor n'ụzọ dabere na ntinye uche. A na-ahụ njikwa BSEP n'elu ụgbọ ala (DMSO) na ntinye uche dị ka 1 nM, ebe a na-ahụ ntinye siri ike nke SHP (15-fold n'elu ụgbọ ala) na 10 nM na ntinye ume nke SHP na 1 nM (3-fold) [1] ].

Ebumnuche: FXR