KATSE # | Lebitso la Sehlahiswa | Tlhaloso |
CPD9470 | Obeticholic acid | Obeticholic Acid (INT747; 6-ECDCA) ke buka e nkiloeng ho cholic acid e sebetsang e le FXR agonist e matla le e khethang e bonts'ang ts'ebetso ea anticholeretic ka har'a mofuta oa in vivo rat oa cholestasis. E thibela ho ruruha ha lisele tsa mesifa ea mesifa le ho falla hammoho le ho khothalletsa phapang ea adipocyte le ho laola tšebetso ea lisele tsa adipose ka vivo. |
CPD100579 | fexaramine | Fexaramine ke agonist ea farnesoid X receptor (FXR), e leng bile acid-activated nuclear receptor e laolang motsoako oa bile-acid synthesis, conjugation le lipalangoang, hammoho le metabolism ea lipid ka liketso sebeteng le maleng. Fexaramine e na le kamano e kholo ka makhetlo a 100 bakeng sa FXR ho feta metsoako ea tlhaho 'me e hlalositse lipakane tsa genomic le sebaka se tlamang ho FXR. Ha e sebelisoa ka molomo ho litoeba, fexaramine e hlahisa liketso tse khethiloeng ka li-receptor tsa FXR ka maleng. |
CPD100577 | Asiti ea Lithocholic | Levallorphan, eo hape e tsejoang ka hore ke levallorphan tartate (USAN), ke modulator ea opioid ea lelapa la morphinan e sebelisoang e le sehlare-bohloko sa opioid le mohanyetsi/antidote ea opioid. E sebetsa e le mohanyetsi oa μ-opioid receptor (MOR) hape e le agonist ea κ-opioid receptor (KOR), ka lebaka leo, e thibela liphello tsa mahlahana a matla a nang le ts'ebetso e kholo ea tlhaho e kang morphine ha ka nako e le 'ngoe e hlahisa analgesia. . Joalo ka agonist ea KOR, levallorphan e ka hlahisa maikutlo a matla a kelello ka litekanyetso tse lekaneng ho kenyelletsa lipono, karohano, le litlamorao tse ling tsa psychotomimetic, dysphoria, matšoenyeho, pherekano, ho tsekela, ho ferekana, ho lahleheloa ke kelello, maikutlo a botahoa le litoro tse makatsang, tse sa tloaelehang kapa tse tšoenyang. . (Mohloli: https://en.wikipedia.org/wiki/Levallorphan). |
CPD100575 | Turofexorate-Isopropyl | Turofexorate isopropyl, eo hape e tsejoang e le WAY-362450 le XL335, ke agonist e matla haholo, e khethang, le ea molomo ea farnesoid X receptor (FXR) (EC (50) = 4 nM, Eff = 149%), e fokotsang ho ruruha ha sebete. le fibrosis ka mohlala oa murine oa steatohepatitis e seng joala |
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,对其他核受体怡有活时。 |
CPD1549 | Tropifexor | Tropifexor ke buka le agonist e matla haholo ea FXR e nang le EC50 ea 0.2 nM. |