2244440-85-3

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
Molecular Formula	C34H43N3O3
Molecular Weight	541.72
MOL File	2244440-85-3.mol

Synonyms

omesdafexor Cyclohexanecarboxamide, N-[3-(1-cyclopropyl-1H-pyrazol-4-yl)phenyl]-4-hydroxy-N-[[trans-4-(4-methoxy-3-methylphenyl)cyclohexyl]methyl]-, trans-

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Chemical Properties

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

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.

Supplier

Shanghai Beckham Medical Technology Co., Ltd

Telephone 13816613772

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList16976/0_EN.htm

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

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