MPAKA # | Dzina lazogulitsa | Kufotokozera |
CPD9470 | Obeticholic acid | Obeticholic Acid (INT747; 6-ECDCA) ndi buku lochokera ku cholic acid yomwe imakhala ngati FXR agonist yamphamvu komanso yosankha yowonetsa anticholeretic zochita mu vivo rat model of cholestasis. Imalepheretsa kutupa kwa maselo osalala a minofu ndi kusamuka komanso kumathandizira kusiyanitsa kwa adipocyte ndikuwongolera magwiridwe antchito a cell adipose mu vivo. |
CPD100579 | fexaramine | Fexaramine ndi agonist wa farnesoid X receptor (FXR), yomwe ndi bile acid-activated nuclear receptor yomwe imayendetsa bile-acid synthesis, conjugation ndi transport, komanso lipid metabolism kudzera m'chiwindi ndi m'matumbo. Fexaramine ili ndi kuyanjana kwakukulu kwa 100 kwa FXR kuposa mankhwala achilengedwe ndipo inafotokoza zolinga za genomic ndi malo omangiriza pa FXR. Ikaperekedwa pakamwa kwa mbewa, fexaramine imapanga zochita zosankhidwa kudzera mu zolandilira za FXR m'matumbo. |
CPD100577 | Lithocholic acid | Levallorphan, yemwe amadziwikanso kuti levallorphan tartate (USAN), ndi modulator wa opioid wa banja la morphinan wogwiritsidwa ntchito ngati opioid analgesic ndi opioid antagonist/antidote. Zimakhala ngati wotsutsa wa μ-opioid receptor (MOR) komanso monga agonist wa κ-opioid receptor (KOR), ndipo chifukwa chake, amalepheretsa zotsatira za othandizira amphamvu omwe ali ndi zochitika zazikulu zamkati monga morphine pamene panthawi imodzimodziyo akupanga analgesia. . Monga agonist wa KOR, levallorphan amatha kubweretsa zovuta zamaganizidwe pamilingo yokwanira kuphatikiza kuyerekezera zinthu m'maganizo, kudzipatula, ndi zina za psychotomimetic zotsatira, dysphoria, nkhawa, chisokonezo, chizungulire, kusokonezeka maganizo, kukhumudwa, kuledzera, ndi zodabwitsa, zachilendo, kapena zosokoneza maloto. . (Kuchokera: https://en.wikipedia.org/wiki/Levallorphan). |
CPD100575 | Turofexorate-Isopropyl | Turofexorate isopropyl, yomwe imadziwikanso kuti WAY-362450 ndi XL335, ndi agonist wamphamvu kwambiri, wosankha, komanso wapakamwa wa farnesoid X receptor (FXR) (EC (50) = 4 nM, Eff = 149%), yomwe imachepetsa kutupa kwa chiwindi. ndi fibrosis mu murine chitsanzo cha non-alcoholic steatohepatitis |
CPD100574 | GW4064 | GW4064是一种farnesoid X receptor (FXR)激动剂,CV1细胞系中EC50為65 nM。浓度达到1 μM时,其他核受体怡有活。 |
Chithunzi cha CPD1549 | Tropifexor | Tropifexor ndi buku komanso agonist wamphamvu kwambiri wa FXR wokhala ndi EC50 ya 0.2 nM. |