Name: TGR5 agonist 10
Brand: TargetMol
SKU: T218011
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

10 mg

待询

10-14周

50 mg

待询

10-14周

生物活性

产品描述	TGR5 agonist 10 is a selective, allosteric, and orally bioavailable agonist for the Takeda G protein-coupled receptor 5 (TGR5), with EC50 values of 0.8 μM for human TGR5 and 0.6 μM for mouse TGR5. It demonstrates specificity for TGR5 over FXR and can activate both human and mouse TGR5 to induce cAMP accumulation. The compound enhances cholic acid's functional activity and efficacy on hTGR5 and shows higher selectivity in cAMP formation compared to β-arrestin 2 recruitment. TGR5 agonist 10 exhibits hypoglycemic effects in an oral glucose tolerance test in Mus musculus and can be utilized in diabetes research.
靶点活性	TGR5 (human):0.8 μM (EC50)
体外活性	TGR5 agonist 10 (compound A1) 对 β-arrestin2 recruitment 的活性较弱（EC 50 = 26.5 μM），低于其在 HEK293T 细胞中促进 cAMP accumulation 的活性。TGR5 agonist 10（10-20 μM；作用 8 小时）在 HEK293T 细胞中于 10 μM 和 20 μM 下均不激活 FXR，提示其对 TGR5 具有选择性。
体内活性	在 ICR 小鼠 OGTT 模型中，TGR5 agonist 10 (compound A1) 经灌胃给药 (100 mg/kg) 后显示出显著的降血糖活性。

化学信息

分子量	436.58
分子式	C₂₅H₄₀O₆
CAS No.	3081614-92-5
Smiles	O(C)[C@H]1[C@]2([C@]3([C@@](C)([C@@]([C@@H](CCC(O)=O)C)(CC3)[H])OC(=O)C[C@@]2([C@]4(C)[C@](C1)(C[C@H](O)CC4)[H])[H])[H])[H]

储存&溶解度

存储	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 实际储存温度请以COA为准

TGR5 agonist 10