Nidufexor (Synonyms: LMB763)
目录号: PL01748 纯度: ≥98%
CAS No. :1773489-72-7
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中文名称
Nidufexor
英文名称
Nidufexor
英文别名
Nidufexor;CJ1PL0TE6J;Nidufexor [INN];BCP28929;4-((N-benzyl-8-chloro-1-methyl-1,4-dihydrochromeno[4,3-c]pyrazole-3-carboxamido)methyl)benzoic acid;Benzoic acid, 4-((((8-chloro-1,4-dihydro-1-methyl(1)benzopyrano(4,3-C)pyrazol-3-yl)carbonyl)(phenylmethyl)amino)methyl)-;LMB763
Cas No.
1773489-72-7
分子式
C27H22ClN3O4
分子量
487.93
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Nidufexor (LMB763) 是一种口服有效的法尼醇 X 受体 (FXR) 激动剂,可用于非酒精性脂肪性肝炎 (NASH) 研究。
生物活性
Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).
性状
Solid
IC50 & Target[1][2]
FXR
体内研究(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.
Nidufexor exhibits moderate C max (4.5, 12.4, 28.1, 80.9, and 140.8 μM) and terminal elimination half-lives (t 1/2 ; 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)
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).
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). has not independently confirmed the accuracy of
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[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.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (170.78 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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