货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V57400-1ml	10mM in DMSO	￥2050.00 V57400-1ml ￥2050.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V57400-1ml

10mM in DMSO

￥2050.00

货期：3-5天

产品描述：

Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran derivative, is a potent oral dipeptidyl aminopeptidase 4 (DPP-4) inhibitor with Long-acting antidiabetic efficacy. Cofrogliptin (compound 2) has a great potential for type 2 diabetes mellitus (T2DM) .

靶点：

DPP-4

体外研究：

Cofrogliptin (HSK7653) (compound 2) (IV: 0.5 mg/kg; PO: 2 mg/kg) exhibits extremely long half-lives and low rate of reduction of drug concentration after orally administration.
Cofrogliptin (compound 2) (Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg) increases of half-lives, has high oral exposure, low i.v. clearance and hepatic microsomal clearance after intravenous dosing.
Cofrogliptin (compound 2) (Single, orally, 10 mg/kg) exhibits longe inhibition time of DPP-4 and decreases HbA1c level
at the doses of 3 and 10 mg/kg in ob/ob mice. Cofrogliptin (compound 2) (Single, orally, 10 mg/kg) also has a great potential of biweekly regimen for T2DM as indicated in rhesus monkeys[2].

Pharmacokinetic Parameters in ICR mice[2]

体内研究：

Cofrogliptin (HSK7653) (compound 2) has the DPP-4 inhibitory activity with an IC50 value of 4.18 nM.

参考文献：

1. International Nonproprietary Names for Pharmaceutical Substances (INN)
2. Chen Zhang, et al. Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. J Med Chem. 2020 Jul 9;63(13):7108-7126.

保存条件：

-80°C 6个月;-20°C 1个月

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.144 ml	10.72 ml	21.439 ml
5 mM	0.429 ml	2.144 ml	4.288 ml
10 mM	0.214 ml	1.072 ml	2.144 ml
50 mM	0.043 ml	0.214 ml	0.429 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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