Gly MCA,FXR拮抗剂

FXR拮抗剂;在肠内有选择性的活性;
  • ≥95%
有货

库存信息

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货号 (SKU) 包装规格 是否现货 价格 数量
G286558-1mg
1mg 期货 Stock Image

基本描述

别名 N-[(3α,5β,6β,7β)-3,6,7-三羟基-24-氧胆烷-24-基]甘氨酸
英文别名 Gly-MCA | GβMCA | Glycine-β-muricholic Acid | N-[(3α,5β,6β,7β)-3,6,7-trihydroxy-24-oxocholan-24-yl]-glycine
规格或纯度 ≥95%
英文名称 Gly MCA
生化机理 法尼醇X受体(FXR)拮抗剂。在回肠中积累并仅在肠道中抑制FXR信号传导。抑制或逆转高脂饮食引起的遗传性肥胖,胰岛素抵抗和小鼠肝脂肪变性。减少肥胖小鼠的肥胖和代谢综合征。
储存温度 -20°C储存
运输条件 超低温冰袋运输
产品介绍


GβMCA is an intestine-selective antagonist of the farnesoid X receptor (FXR) and the glycine-conjugatedform of the murine-specific primary bile acid β-muricholic acid (Item No. 20287).1,2 It inhibits expression ofthe FXR target genes Shp and Fgf15 induced by the FXR ligands chenodeoxycholic acid (Item No. 10011286)and GW 4064 (Item No. 10006611) in Caco-2 cells when used at a concentration of 100 μM. GβMCA isresistant to hydrolysis by fecal bile salt hydrolase (BSH) isolated from gut microbiota, indicating gut stability.Dietary administration of GβMCA (10 mg/kg) decreases Shp and Fgf15 mRNA expression in ileum, but notliver, and reduces ceramide levels and expression of the ceramide synthesis-related genes Sptlc2, Sptlc3,Cers2, Cers4, Degs1, Degs2, Smpd3, and Smpd4 in ileum of mice with high-fat diet-induced obesity and db/dbmice. It also prevents weight gain, reduces blood glucose levels, and increases insulin sensitivity as well asprevents development of cholestasis and necrotic lesions in liver of mice with high-fat diet-induced obesity.

AI解读

名称和识别符

IUPAC Name 2-[[(4R)-4-[(3R,5R,6S,7R,10R,13R)-3,6,7-trihydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]pentanoyl]amino]acetic acid
INCHI InChI=1S/C26H43NO6/c1-14(4-7-20(29)27-13-21(30)31)16-5-6-17-22-18(9-11-25(16,17)2)26(3)10-8-15(28)12-19(26)23(32)24(22)33/h14-19,22-24,28,32-33H,4-13H2,1-3H3,(H,27,29)(H,30,31)/t14-,15-,16?,17?,18?,19+,22?,23+,24-,25-,26-/m1/s1
InChi Key ZQYUKJFJPJDMMR-DLUUSONCSA-N
Canonical SMILES CC(CCC(=O)NCC(=O)O)C1CCC2C1(CCC3C2C(C(C4C3(CCC(C4)O)C)O)O)C
PubChem CID 131675923
分子量 465.62

化学和物理性质

溶解性 DMF: 30 mg/ml;DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml;DMSO: 20 mg/ml;Ethanol: 20 mg/ml

安全和危险性(GHS)

技术规格说明书

NMR Spectrum 1H Conforms to Structure
LC-MS for identification Conforms
Purity(HPLC area)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器