CAT # | Igama lemveliso | Inkcazo |
CPD9470 | I-Obeticholic-Acid | I-Obeticholic Acid (INT747; 6-ECDCA) iyinoveli ephuma kwi-cholic acid esebenza njenge-agonist enamandla kwaye ekhethiweyo ye-FXR ebonisa umsebenzi we-anticholeretic kwi-vivo rat model ye-cholestasis. Ivimbela ukuvutha kweeseli ze-vascular smooth muscle kunye nokufuduka kunye nokukhuthaza ukuhlukana kwe-adipocyte kwaye ilawula ukusebenza kweeseli ze-adipose kwi-vivo. |
CPD100579 | fexaramine | I-Fexaramine i-agonist ye-farnesoid X receptor (FXR), eyi-bile acid-activated nuclear receptor elawula i-bile-acid synthesis, i-conjugation kunye nokuthutha, kunye ne-lipid metabolism ngezenzo kwisibindi kunye namathumbu. I-Fexaramine ine-100-fold-fold-affinity enkulu ye-FXR kuneekhompawundi zendalo kwaye ichaze iithagethi ze-genomic kunye nesayithi lokubopha kwi-FXR. Xa ilawulwa ngomlomo kwiigundane, i-fexaramine yavelisa izenzo ezikhethiweyo ngokusebenzisa i-FXR receptors emathunjini. |
CPD100577 | I-Lithocholic acid | I-Levallorphan, eyaziwa ngokuba yi-levallorphan tartate (USAN), i-opioid modulator yentsapho ye-morphinan esetyenziswa njenge-opioid analgesic kunye ne-opioid antagonist/antidote. Isebenza njengomchasi we-μ-opioid receptor (MOR) kunye ne-agonist ye-κ-opioid receptor (KOR), kwaye ngenxa yoko, ivimbela imiphumo yee-agent ezinamandla ezinomsebenzi omkhulu we-intrinsic njenge-morphine ngelixa ngaxeshanye ivelisa i-analgesia. . Njenge-agonist ye-KOR, i-levallorphan inokuvelisa ukuphendulwa kwengqondo okuqatha kwidosi eyaneleyo kubandakanya i-hallucinations, ukwahlukana, kunye nezinye iziphumo ze-psychotomimetic, i-dysphoria, ixhala, ukudideka, isiyezi, ukudideka, ukungaziqondi, iimvakalelo zokunxila, kunye namaphupha angaqhelekanga, angaqhelekanga, okanye aphazamisayo. . (Umthombo: https://en.wikipedia.org/wiki/Levallorphan). |
CPD100575 | I-Turofexorate-Isopropyl | I-Turofexorate isopropyl, eyaziwa ngokuba yi-WAY-362450 kunye ne-XL335, i-agonist enamandla kakhulu, ekhethiweyo, kunye neyomlomo esebenzayo ye-farnesoid X receptor (FXR) (EC (50) = 4 nM, Eff = 149%), enciphisa ukuvuvukala kwesibindi. kunye ne-fibrosis kwimodeli ye-murine ye-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,其他核受体沒有活。 |
CPD1549 | Tropifexor | I-Tropifexor yinoveli kunye ne-agonist enamandla kakhulu yeFXR ene-EC50 ye-0.2 nM. |