574013-66-4
中文名稱
FEXARAMINE
英文名稱
Fexaramine
CAS
574013-66-4
分子式
C32H36N2O3
分子量
496.64
MOL 文件
574013-66-4.mol
更新日期
2024/11/08 11:24:22
574013-66-4 結構式
基本信息
中文別名
3-[3-[(環(huán)己基羰基)[[4'-(二甲基氨基)[1,1'-聯(lián)苯]-4-基]甲基]氨基]苯基]-2-丙烯酸甲酯3-[3-[(環(huán)己基羰基)[[4\'-(二甲基氨基)[1,1\'-聯(lián)苯]-4-基]甲基]氨基]苯基]-2-丙烯酸甲酯, >98%
英文別名
CS-1691Fexaramine
3-[3-[(Cyclohexylcarbonyl)-[[4'-(dimethylamino)-[1,1'-biphenyl]-4-yl]methyl]amino]phenyl]-2-pr
(E)-methyl 3-(3-(N-((4'-(dimethylamino)biphenyl-4-yl)methyl)cyclohexanecarboxamido)phenyl)acrylate
3-[3-[(Cyclohexylcarbonyl)-[[4'-(dimethylamino)-[1,1'-biphenyl]-4-yl]methyl]amino]phenyl]-2-propenoicacidmethylester
2-Propenoic acid, 3-[3-[(cyclohexylcarbonyl)[[4'-(diMethylaMino)[1,1'-biphenyl]-4-yl]Methyl]aMino]phenyl]-, Methyl ester
3-[3-[(Cyclohexylcarbonyl)[[4\'-(dimethylamino)[1,1\'-biphenyl]-4-yl]methyl]amino]phenyl]-2-Propenoic acid methyl ester, >98%
2-Propenoic acid, 3-[3-[(cyclohexylcarbonyl)[[4'-(dimethylamino)[1,1'-biphenyl]-4-yl]methyl]amino]phenyl]-, methyl ester, (2E)-
(2E,4Z)-5-(3-(N-((4'-(dimethylamino)biphenyl-4-yl)methyl)cyclohexanecarboxamido)phenyl)-4-(methoxycarbonyl)penta-2,4-dienoic acid
所屬類別
生物化工：激動劑抑制劑物理化學性質
沸點677.7±55.0 °C(Predicted)
密度1.158±0.06 g/cm3(Predicted)
儲存條件2-8°C
溶解度DMSO : 50 mg/mL (100.68 mM; Need ultrasonic)
酸度系數(pKa)4.95±0.24(Predicted)
形態(tài)粉末
顏色白色至米色
常見問題列表
生物活性
Fexaramine是一種有效的、選擇性farnesoid X receptor (FXR)激動劑，EC50為25 nM。它對hRXRα, hPPARα, hPPARγ, hPPARδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ和hVDR受體沒有活性。靶點
| Target | Value |
|
FXR
() | 25 nM(EC50) |
體外研究
Bile acid treatment is performed in HuTu-80 cells with Fexaramine (5, 25, and 50 μM) for 24 h. Fexaramine (50 μM) increases small heterodimer partner (SHP) transcript levels by 2.1-fold. The cells are treated with various concentrations of Fexaramine, and the endogenous secretin transcript levels are significantly reduced (33% in 50 μM Fexaramine). Fexaramine treatment also significantly suppresses secretin promoter activity by 32%.
體內研究
Fexaramine treatment of DIO mice produces a striking metabolic profile that includes reduced weight gain, decreased inflammation, browning of WAT and increased insulin sensitization.