I-FXR

IKATI # Igama Lomkhiqizo Incazelo
CPD9470 I-Obeticholic Acid I-Obeticholic Acid (INT747; 6-ECDCA) iyinoveli esuselwe ku-cholic acid esebenza njenge-FXR agonist enamandla futhi ekhethiwe ebonisa umsebenzi we-anticholeretic kumodeli ye-in vivo rat ye-cholestasis. Ivimbela ukuvuvukala kwe-vascular smooth cell cell kanye nokufuduka kanye nokukhuthaza ukuhlukaniswa kwe-adipocyte futhi ilawula ukusebenza kwe-adipose cell ku-vivo.
I-CPD100579 i-fexaramine I-Fexaramine iyi-agonist ye-farnesoid X receptor (FXR), okuyi-bile acid-activated nuclear receptor elawula ukuhlanganiswa kwe-bile-acid, ukuhlanganiswa nokuthutha, kanye ne-lipid metabolism ngezenzo esibindini nasemathunjini. I-Fexaramine inobudlelwane obukhulu obuphindwe izikhathi eziyi-100 ku-FXR kunezinhlanganisela zemvelo futhi yachaza izinhloso ze-genomic kanye nesayithi elibophayo ku-FXR. Lapho inikezwa ngomlomo kumagundane, i-fexaramine ikhiqiza izenzo ezikhethiwe ngokusebenzisa ama-FXR receptors emathunjini.
I-CPD100577 I-Lithocholic acid I-Levallorphan, eyaziwa nangokuthi i-levallorphan tartate (USAN), iyimoduli ye-opioid yomndeni we-morphinan esetshenziswa njenge-opioid analgesic kanye ne-opioid antagonist/antidote. Isebenza njengomphikisi we-μ-opioid receptor (MOR) futhi njenge-agonist ye-κ-opioid receptor (KOR), futhi ngenxa yalokho, ivimbela imiphumela yama-ejenti anamandla anomsebenzi omkhulu wangaphakathi njenge-morphine ngenkathi ngesikhathi esifanayo ikhiqiza i-analgesia. . Njenge-agonist ye-KOR, i-levallorphan ingakhiqiza ukusabela kwengqondo okunamandla ngemithamo eyanele okuhlanganisa ukubona izinto ezingekho, ukuhlukaniswa, neminye imiphumela ye-psychotomimetic, i-dysphoria, ukukhathazeka, ukudideka, isiyezi, ukudideka, ukudangala, imizwa yokudakwa, namaphupho ayinqaba, angajwayelekile, noma aphazamisayo. . (Umthombo: https://en.wikipedia.org/wiki/Levallorphan).
I-CPD100575 I-Turofexorate-Isopropyl I-Turofexorate isopropyl, eyaziwa nangokuthi i-WAY-362450 ne-XL335, iyi-agonist enamandla kakhulu, ekhethayo, futhi esebenza ngomlomo ye-farnesoid X receptor (FXR) (EC(50) = 4 nM, Eff = 149%), enciphisa ukuvuvukala kwesibindi. kanye ne-fibrosis kumodeli ye-murine ye-non-alcohol steatohepatitis
I-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。
I-CPD1549 I-Tropifexor I-Tropifexor iyinoveli futhi i-agonist enamandla kakhulu ye-FXR ene-EC50 ye-0.2 nM.
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