Name: Safiglipron
Brand: TargetMol
SKU: T204742
Price: 3250 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

1 mg

¥ 1,300

现货

5 mg

¥ 3,250

现货

10 mg

待询

现货

25 mg

待询

现货

50 mg

待询

100 mg

待询

生物活性

产品描述	Safiglipron is a small molecule GLP-1 receptor agonist that mimics the incretin effect by activating the GLP-1 receptor, with a half-maximal effective concentration (EC₅₀) of 0.74 nM against the human GLP-1 receptor, demonstrating strong agonistic activity. Additionally, Safiglipron has a half-maximal inhibitory concentration (IC₅₀) of 10.1 μM against the hERG potassium channel. Safiglipron is suitable for diabetes research.
靶点活性 (IC₅₀)	K+ channel (hERG):10.1 μM, GLP1 receptor:0.74 nM (EC₅₀)
体外活性	方法：Safiglipron（该研究使用编号Example 4）在GLP-1 receptor功能性报告实验中进行评价。结果：Example 4激活GLP-1 receptor信号，EC₅₀为0.74 nM，Emax为103%。^[1] 方法：Safiglipron（该研究使用编号Example 4）在稳定表达hERG的细胞中采用手动膜片钳实验检测hERG钾电流。结果：Example 4抑制hERG电流，IC₅₀为10.1 μM。^[1]
体内活性	方法：Safiglipron（该研究使用编号Example 4）以2 mg/kg口服给予雌性C57小鼠，并采用LC-MS/MS测定血浆浓度。结果：口服给药后Example 4的Cmax为797 ng/mL，AUC0-t为2247 ng·h/mL，终末半衰期约3.1 h。^[1]
别名	GLP-1 receptor agonist 15

化学信息

分子量	592.06
分子式	C₃₂H₃₁ClFN₃O₅
CAS No.	2757506-39-9
Smiles	C(N1C=2C(N=C1CN3CCC(CC3)C4=C5C(OC[C@@H](O5)C6=C(F)C=C(Cl)C=C6)=CC=C4)=CC=C(C(O)=O)C2)[C@@H]7CCO7

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

Safiglipron