| Identification | Back Directory | [Name]
4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid | [CAS]
1773489-72-7 | [Synonyms]
LMB-763
CS-2689
Nidufexor
EOS-61760
Nidufexor(LMB-763)
(Nidufexor)EOS-61760
4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoicacid
Benzoic acid, 4-[[[(8-chloro-1,4-dihydro-1-methyl[1]benzopyrano[4,3-c]pyrazol-3-yl)carbonyl](phenylmethyl)amino]methyl]- | [Molecular Formula]
C27H22ClN3O4 | [MDL Number]
MFCD31657267 | [MOL File]
1773489-72-7.mol | [Molecular Weight]
487.93 |
| Chemical Properties | Back Directory | [Boiling point ]
781.1±60.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: soluble; Ethanol: soluble | [form ]
A solid | [pka]
4.17±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH)[1]. | [in vivo]
Nidufexor (LMB763) is a potent and specific FXR-gene modulator in vivo, reducing steatosis, inflammation and fibrosis in nonalcoholic steatohepatitis (NASH) murine models[1].
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Nidufexor exhibits moderate Cmax (4.5, 12.4, 28.1, 80.9, and 140.8 μM) and terminal elimination half-lives (t1/2; 3.9 5.7 6.3 5.6 6.3 h) following oral administration (3 ,10 ,30, 100, and 300mg/kg) in adult male Wistar Han rats (age approximately 10 weeks)[1]
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Nidufexor exhibits terminal elimination half-lives (mouse 4.5, rat 4.4 and, dog 6.8 h) following intravenous administration (mouse 3.0, rat 5.0 and, dog 0.5 mg/kg)[1].
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Nidufexor exhibits terminal elimination half-lives (mouse 3.5, rat 2.7 and, dog 10.1 h) following oral administration (mouse 10, rat 10 and, dog 2 mg/kg)[1]. | Animal Model: | Han-Wistar rats[1] | | Dosage: | 0.1, 0.3, 1.5, 7.5, 25, 100 mg/kg (Pharmacokinetic Analysis) | | Administration: | Oral gavage, once daily for 14 days | | Result: | On day 1 and 13, serum exposure increased approximately dose-proportionally from 0.1 to 100 mg/kg. Exposure at 0.1 and 0.3 mg/kg was likely underestimated on day 13. No significant accumulation was observed[1]. |
| [References]
[1] Chianelli D, et al. Nidufexor (LMB763), a Novel FXR Modulator for the Treatment of Nonalcoholic Steatohepatitis. J Med Chem. 2020 Apr 23;63(8):3868-3880. DOI:10.1021/acs.jmedchem.9b01621 |
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