TGR5 Receptor Agonist
| EC | EINECS 200-256-5 |
| MDL | MFCD17169972 |
| 别名 | 3-(2-氯苯基)-n-(4-氯苯基)-n,5-二甲基-4-异f唑羧酰胺 |
| 英文名称 | TGR5 Receptor Agonist |
| CAS | 1197300-24-5 |
| 分子式 | C18H14Cl2N2O2 |
| 分子量 | 361.22 |
| 纯度 | Purity≥99% |
| 单位 | 支 |
| SMILES | ClC1=CC=CC=C1C2=NOC(C)=C2C(N(C)C3=CC=C(Cl)C=C3)=O |
| 靶点 | GPCR19 |
| 规格 | 5mg 10mg |
INT-767
| 含量 | Purity≥98% |
| CAS | 1000403-03-1 |
| 分子式 | C25H43NaO6S |
| 分子量 | 494.66 |
| 纯度 | ≥98% |
| 单位 | 支 |
| 生物活性 | INT-767是法尼醇X受体/TGR5双激动剂，平均 EC50 分别为30和630 nM。INT-767 是一种安全有效的 FXR 和 TGR5 依赖性途径的调节剂。[1-2] |
| In Vitro | INT-767 is a potent agonist for both FXR (mean EC(50), 30 nM by PerkinElmer AlphaScreen assay) and TGR5 (mean EC(50), 630 nM by time resolved-fluorescence resonance energy transfer). INT-767 does not show cytotoxic effects in HepG2 cells. INT-767 induces FXR-dependent lipid uptake by adipocytes, with the beneficial effect of shuttling lipids from central hepatic to peripheral fat storage, and promotes TGR5-dependent glucagon-like peptide-1 secretion by enteroendocrine cells, a validated target in the treatment of type 2 diabetes. [2] |
| In Vivo | Only the dual FXR/TGR5 agonist, INT-767, significantly improved serum liver enzymes, hepatic inflammation, and biliary fibrosis in Mdr2(-/-) mice. In line with this, INT-767 significantly induced bile flow and biliary HCO 3- output, as well as gene expression of carbonic anhydrase 14, an important enzyme able to enhance HCO 3- transport, in an Fxr-dependent manner. In addition, INT-767 dramatically reduced bile acid synthesis via the induction of ileal Fgf15 and hepatic Shp gene expression, thus resulting in significantly reduced biliary bile acid output in Mdr2(-/-) mice.[1] INT-767 treatment markedly decreases cholesterol and triglyceride levels in diabetic db/db mice and in mice rendered diabetic by streptozotocin administration. [2] |
| SMILES | C[C@H](CCOS(=O)([O-])=O)[C@@]1([H])CC[C@@]2([H])[C@]3([H])[C@H](O)[C@H](CC)[C@]4([H])C[C@H](O)CC[C@]4(C)[C@@]3([H])CC[C@@]21C.[Na+] |
| 靶点 | FXR |
| 数据来源文献 | [1]. Baghdasaryan A, et al. Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mousecholangiopathy model by promoting biliary HCO3- output. Hepatology. 2011 Oct;54(4):1303-1312. [2]. Rizzo G, et al. Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor andTGR5 agonist. Mol Pharmacol. 2010 Oct;78(4):617-630. |
| 规格 | 5mg |
是一种G-protein coupled/Farnesoid X-activated receptor激动剂