This is a demo store. No orders will be fulfilled.

鹅去氧胆酸(CDCA), 胆汁酸受体 FXR 激动剂

FXR Agonists
  • CAS编号: 474-25-9
  • 分子式: C24H40O4
  • 分子量: 392.58
有货

库存信息

关闭
货号 (SKU) 包装规格 是否现货 价格 数量
C408499-1ml
1ml 现货 Stock Image
查看相关系列
Compound libraries (12333)

基本描述

英文别名 Chenodiol | (3α,​5β,​7α)​-3,​7-​dihydroxy-cholan-​24-​oic acid
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Chenodeoxycholic Acid(CDCA)
生化机理 Chenodeoxycholic Acid(Chenodiol)是一种天然存在的人体胆汁酸,可抑制胆固醇在肝脏中的生成和在肠道中的吸收。Chenodeoxycholic Acid 是一种疏水性初级胆汁酸,可激活参与胆固醇代谢的核受体 (FXR)。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 激动剂
作用机制 胆汁酸受体 FXR 激动剂
产品介绍

Chenodeoxycholic Acid, Free Acid and its 7β-isomer ursodeoxycholic acid are potent (nanomolar affinity) selective inhibitors of DD2 (AKR1C2). These compounds were non-competitive inhibitors of AKR1D1 yielding Ki values of 3.2 μM for chenodeoxycholic acid. This chemical is a hydrophobic primary bile acid, which increases intracellular Ca2+ in rat hepatocyte couplets. Studies indicate that Chenodeoxycholic Acid induces apoptosis throμgh a PKC dependent pathway. It is known that Chenodeoxycholic Acid is essential in the metabolism of cholesterol via activation of nuclear receptors. This bile acid can also bind to BABP with a stoichiometery of 1:2. Alternate studies indicate that chenodeoxycholic acid can inhibit the expression of IL-6 and cell viability in QBC939 cells.An apoptosis inducer via PKC-dependent signalling pathway.

Information

Chenodeoxycholic Acid Chenodeoxycholic Acid (Chenodiol) is a naturally occurring human bile acid, and inhibits production of cholesterol in the liver and absorption in the intestines. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activat
In vitro

Chenodeoxycholic acid (CDCA) and Deoxycholic acid (DCA) both inhibits 11 beta HSD2 with IC(50) values of 22 mM and 38 mM, respectively and causes cortisol-dependent nuclear translocation and increases transcriptionalactivity of mineralocorticoid receptor (MR). Chenodeoxycholic acid is able to stimulate Ishikawa cell growth by inducing a significant increase in Cyclin D1 protein and mRNA expression through the activation of the membrane G protein-coupled receptor (TGR5)-dependent pathway. Chenodeoxycholic acid (CDCA) induces LDL receptor mRNA levels approximately 4 fold and mRNA levels for HMG-CoA reductase and HMG-CoA synthase two fold in a cultured human hepatoblastoma cell line, Hep G2. Chenodeoxycholic acid-induced Isc is inhibited (≥67%) by Bumetanide, BaCl2, and the cystic fibrosis transmembrane conductance regulator (CFTR) inhibitor CFTRinh-172. Chenodeoxycholic acid-stimulated Isc is decreased 43% by the adenylate cyclase inhibitor MDL12330A and Chenodeoxycholic acid increases intracellular cAMP concentration. Chenodeoxycholic acid treatment activates C/EBPβ, as shown by increases in its phosphorylation, nuclear accumulation, and expression in HepG2 cells. Chenodeoxycholic acid enhances luciferase gene transcription from the construct containing -1.65-kb GSTA2 promoter, which contains C/EBP response element (pGL-1651). Chenodeoxycholic acid treatment activates AMP-activated protein kinase (AMPK), which leads to extracellular signal-regulated kinase 1/2 (ERK1/2) activation, as evidenced by the results of experiments using a dominant-negative mutant of AMPKα and chemical inhibitor.

In vivo


Cell Data

cell lines:

Concentrations:

Incubation Time:

Powder Purity:≥99%

产品属性

ALogP 4.9

关联靶点(人)

FPR1 Tchem fMet-Leu-Phe 受体(fMet-Leu-Phe receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
NR1H4 Tclin 胆汁酸受体(Bile acid receptor) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
GPBAR1 Tchem G蛋白偶联胆汁酸受体1(G-protein coupled bile acid receptor 1) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES C[C@H](CCC(=O)O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2[C@@H](C[C@H]4[C@@]3(CC[C@H](C4)O)C)O)C
分子量 392.58
Reaxy-Rn 2820380
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2820380&ln=

化学和物理性质

溶解性 Solubility (25°C) In vitro      

安全和危险性(GHS)

Merck Index 2054

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