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) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，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
-80℃储存。特低温运输 。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 5 篇同行评审文献引用。
概述
Vildagliptin is a dipeptidyl peptidase-4 (CD26) inhibitor. CD26 activates serine proteases in immune/inflammatory cells. Vildagliptin also inhibits dipeptidyl-peptidase 8 (DPRP1) and dipeptidyl-peptidase 9 (DPRP2), which have been correlated to T cell activation and immune function, as well as diabetes and cancer regulation.A CD26 inhibitor associated with immune response inhibition
Information
Vildagliptin (LAF-237) Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.
In vitro
Vildagliptin is the most stable DPP-IV inhibitor, binding in the S1- and S2-catalytic sites of DPP-IV, possessing a P-1 site transition-state mimetic.
In vivo
Vildagliptin(orally dosed with 10 μmol/kg) is a potent, orally active inhibitor of plasma DPP-IV activity that provides increased levels of GLP-1 in an oral glucose tolerance test (OGTT) with Obese male Zucker rats. Vildagliptin orally dosed with 10 μmol/kg both significantly decreases glucose excursions and stimulates insulin secretion in Obese male Zucker rats. Maximum inhibition of plasma DPP-IV activity (95%) is observed approximately 2 hours postdose of Vildagliptin (1 μmol/kg, po) while >50% inhibition of DPP-IV is observed within 30 min postdose and persisted for >10 hours in normal Cynomolgus monkeys. Vildagliptin(60 mg/kg) increases pancreatic beta cell mass through enhanced beta cell replication and reduced apoptosis, and the increased beta cell mass is sustained for 12 days after vildagliptin washout. Vildagliptin administrated at doses of 10 mg/kg for 32 weeks protects nerve fiber loss in streptozotocin (STZ)-induced diabetic adult male Sprague Dawley rats.
Cell Data
cell lines：MCF7, NCI-H292, Colo-205, HT29, H358, H1703, BxPC3, A673, SW620, DU4475, HepG2 and Hepa-1, RKO 3T3/hulGF-IR and H292 cells
Concentrations：
Incubation Time：
Powder Purity:≥99%
规格
别名
维达列汀（LAF-237）
英文别名
2-Pyrrolidinecarbonitrile, 1-[2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-, (2S)-
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Vildagliptin (LAF-237)
生化机理
维达列汀（LAF-237）抑制 DPP-4 的 IC50 为 2.3 nM。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
二肽基肽酶 IV 抑制剂
名称和识别符
EC号
630-410-0
分子类型
小分子
Isomeric SMILES
C1C[C@H](N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N
PubChem CID
分子量
303.4
技术文档
高级数据
产品属性
| ALogP | 0.9 |
|---|
关联靶点（人）
DPP4
Tclin
二肽基肽酶4(Dipeptidyl peptidase 4)
(36 活性数据)
DPP8
Tchem
二肽基肽酶 8(Dipeptidyl peptidase 8)
(2 活性数据)
DPP9
Tchem
二肽基肽酶9(Dipeptidyl peptidase 9)
(12 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 50 mg/mL (61.6 mM);
安全和危险性（GHS）
危险声明
H413: 可能对水生生物造成长期的有害影响
预防措施声明
P273: 避免释放到环境中。
P501: 将内容物/容器处理到。。。
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:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 C2310997 |
分析证书 | V408745 |
技术文档和文章
此产品的引用文献
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。
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