CAT # | Khoom npe | Kev piav qhia |
PAB 9470 | Obeticholic-Acid | Obeticholic Acid (INT747; 6-ECDCA) yog ib qho tshiab derivative ntawm cholic acid uas ua raws li lub zog thiab xaiv FXR agonist nthuav tawm cov kev ua haujlwm anticholeretic hauv vivo nas qauv ntawm cholestasis. Nws inhibits vascular du leeg cell o thiab tsiv teb tsaws thiab txhawb nqa adipocytes sib txawv thiab tswj adipose cell muaj nuj nqi hauv vivo. |
PAB 100579 | fexaramine | Fexaramine yog ib qho agonist ntawm farnesoid X receptor (FXR), uas yog cov kua tsib acid-activated nuclear receptor uas tswj cov kua tsib-acid synthesis, conjugation thiab thauj, nrog rau lipid metabolism los ntawm kev ua hauv daim siab thiab txoj hnyuv. Fexaramine muaj 100-fold ntau dua affinity rau FXR dua li tej yam ntuj tso tebchaw thiab piav txog lub hom phiaj genomic thiab khi qhov chaw ntawm FXR. Thaum muab tshuaj rau cov nas, fexaramine tsim cov kev xaiv los ntawm FXR receptors hauv cov hnyuv. |
PAB 100577 | Lithocholic-acid | Levallorphan, tseem hu ua levallorphan tartate (USAN), yog opioid modulator ntawm tsev neeg morphinan siv los ua opioid analgesic thiab opioid antagonist / antidote. Nws ua raws li tus antagonist ntawm μ-opioid receptor (MOR) thiab ua tus agonist ntawm κ-opioid receptor (KOR), thiab vim li ntawd, thaiv cov teebmeem ntawm cov neeg ua haujlwm muaj zog nrog ntau dua cov haujlwm hauv lub cev xws li morphine thaum lub sijhawm ua kom muaj kev ua xua. . Raws li tus agonist ntawm KOR, levallorphan tuaj yeem ua rau muaj kev puas siab puas ntsws loj ntawm cov koob tshuaj txaus suav nrog kev hnov lus, kev tsis sib haum xeeb, thiab lwm yam kev puas siab puas ntsws, dysphoria, ntxhov siab, tsis meej pem, kiv taub hau, disorientation, derealization, kev xav qaug dej qaug cawv, thiab txawv txawv, txawv txawv, lossis kev npau suav phem. . (Source: https://en.wikipedia.org/wiki/Levallorphan). |
PIB 100575 | Turofexorate-Isopropyl | Turofexorate isopropyl, tseem hu ua WAY-362450 thiab XL335, yog lub zog muaj zog, xaiv, thiab hais lus nquag agonist ntawm farnesoid X receptor (FXR) (EC(50) = 4 nM, Eff = 149%), uas ua rau lub siab mob. thiab fibrosis hauv murine qauv ntawm non-alcoholic steatohepatitis |
PIB 100574 | wb 4064 | GW4064是一种farnesoid X receptor (FXR) 激动剂,CV1细胞系中EC50为65 nM。浓度达到1 μM时,对其有核受体 |
PAB 1549 | Tropifexor | Tropifexor yog ib qho tshiab thiab muaj zog agonist ntawm FXR nrog EC50 ntawm 0.2 nM. |