计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-20°C储存。超低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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)
In Vitro
Cofrogliptin (HSK7653) (compound 2) has the DPP-4 inhibitory activity with an IC 50 value of 4.18 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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\nat 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. Pharmacokinetic Parameters in ICR miceIV(dose: 0.5 mg/kg) PO(dose: 2 mg/kg) CI(mL/min/kg) V dss (L/kg) t 1/2 (h) C max (ng/mL) t 1/2 (h) AUC 0-t (ng•h/mL) F% Omarigliptin 7.39±2.1 1.65±0.27 3.05±0.6 798±122 4.65±1.4 4095±552 95.0±29 Cofrogliptin (compound 2) 2.57±0.09 3.30±0.33 25.6±9.6 352±20 29.9±3.2 7898±873 62.2±6.9 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: ob/ob miceDosage: 3 mg/kg, 10 mg/kg, 30 mg/kg Administration: Single, orally, 3 mg/kg, 10 mg/kg, 30 mg/kg Result: Exhibited strong inhibition capability of plasma DPP-4 in a dose dependent manner. Animal Model: rhesus monkeysDosage: 10 mg/kg Administration: Single, orally, 10 mg/kg Result: Possessed the capability of plasma DPP-4 inhibition over 80% for at least 12 days. Remained the plasma DPP-4 inhibition rates of 76.16% and 43.41%, respectively at the end of second week and third week after administration.
Form:Solid
IC50& Target:DPP-4
规格
别名
考罗列汀
规格或纯度
≥99%
英文名称
Cofrogliptin
生化机理
Cofrogliptin (HSK7653)（化合物 2）是一种四氢吡喃衍生物，是一种强效口服二肽基氨肽酶 4 (DPP-4) 抑制剂，具有长效抗糖尿病功效。Cofrogliptin （化合物 2）具有治疗 2 型糖尿病（T2DM）的巨大潜力[......]。
储存条件
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
Isomeric SMILES
CS(=O)(=O)N1C=C2CN(CC2=N1)[C@@H]3C[C@@H]([C@H](O[C@@H]3C(F)(F)F)C4=C(C=CC(=C4)F)F)N
PubChem CID
分子量
466.43
技术文档
高级数据
关联靶点（人）
DPP4
Tclin
二肽基肽酶4(Dipeptidyl peptidase 4)
(1 活性数据)
KCNH2
Tclin
HERG
(29587 活性数据)
CYP2C8
Tchem
Cytochrome P450 2C8
(1492 活性数据)
CYP2D6
Tclin
Cytochrome P450 2D6
(33882 活性数据)
CYP1A2
Tchem
Cytochrome P450 1A2
(26471 活性数据)
CYP3A5
Tclin
Cytochrome P450 3A5
(525 活性数据)
CYP2C9
Tchem
Cytochrome P450 2C9
(32119 活性数据)
CYP2C19
Tchem
Cytochrome P450 2C19
(29246 活性数据)
CYP3A4
Tclin
Cytochrome P450 3A4
(53859 活性数据)
CYP2E1
Tchem
Cytochrome P450 2E1
(2174 活性数据)
CYP2A6
Tchem
Cytochrome P450 2A6
(2861 活性数据)
CYP2B6
Tchem
Cytochrome P450 2B6
(1338 活性数据)
DPP8
Tchem
Dipeptidyl peptidase VIII
(2139 活性数据)
DPP9
Tchem
Dipeptidyl peptidase IX
(1624 活性数据)
关联靶点（其它种属）
DPP4
Dipeptidyl peptidase IV (11 活性数据)
Mus musculus (284745 活性数据)
Rhesus monkey (3147 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 100 mg/mL (214.39 mM; Need ultrasonic)
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
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
Copyright © 2023至今 上海阿拉丁生化科技股份有限公司 保留所有权利。
危险品化学品经营许可证（带存储）