| Identification | Back Directory | [Name]
Cyclohexanecarboxamide, N-[3-(1-cyclopropyl-1H-pyrazol-4-yl)phenyl]-4-hydroxy-N-[[trans-4-(4-methoxy-3-methylphenyl)cyclohexyl]methyl]-, trans- | [CAS]
2244440-85-3 | [Synonyms]
omesdafexor
Cyclohexanecarboxamide, N-[3-(1-cyclopropyl-1H-pyrazol-4-yl)phenyl]-4-hydroxy-N-[[trans-4-(4-methoxy-3-methylphenyl)cyclohexyl]methyl]-, trans- | [Molecular Formula]
C34H43N3O3 | [MOL File]
2244440-85-3.mol | [Molecular Weight]
541.72 |
| Chemical Properties | Back Directory | [Boiling point ]
735.5±60.0 °C(Predicted) | [density ]
1.24±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
14.96±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Omesdafexor (MET642) is an oral FXR agonist. Omesdafexor can improve colitis induced by adoptive T cell transfer，promote intestinal antimicrobial function, barrier function and inhibit inflammation [1][2][3]. | [in vivo]
Omesdafexor (0.03-0.3 mg/kg, orally, once daily, four weeks) with tofacitinib can synergistically improve colitis[2].
Omesdafexor (0.1-1 mg/kg, orally, once daily, four weeks) can improve colitis induced by adoptive T cell transfer[3]. | Animal Model: | Colitis mouse model [2] | | Dosage: | 0.03, 0.3 mg/kg; once a day; four weeks | | Administration: | Oral | | Result: | Reduced the number of innate immune cells in mesenteric lymph nodes, but not T cells, and could synergistically improve colitis when used in combination with tofacitinib. |
| Animal Model: | Transplanting CD4+CD45RBhi T-cells to recipient C.B-17 SCID mice[3] | | Dosage: | 0.1, 0.3, 1 mg/kg; once a day; four weeks | | Administration: | Oral | | Result: | Improved adoptive T cell transfer-induced colitis, promoted intestinal antimicrobial function, barrier function and inhibited inflammation. |
| [References]
[1] https://cdn.who.int/media/docs/default-source/international-nonproprietary-names-(inn)/pl127.pdf?sfvrsn=8544ca1e_3&download=true
[2] Xueqing Liu, et al. COMBINATION OF FXR AGONIST MET642 WITH TOFACITINIB EXHIBITS SYNERGISTIC EFFECTS IN IMPROVING COLITIS IN ADOPTIVE T-CELL TRANSFER IBD MODEL. METACRINE.
[3] Xueqing Liu, et al. P153 MET642, AN ORAL FXR AGONIST, IMPROVES COLITIS INDUCED BY ADOPTIVE T-CELL TRANSFER. Volume 158, Issue 3, Supplement S11February 2020. |
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