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| 品牌 | absin | CAS | 274901-16-5 |
|---|---|---|---|
| 分子式 | C17H25N3O2 | 纯度 | ＞98% |
| 分子量 | 303.4 | 货号 | abs47027730 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a new oral anti-hyperglycemic agent | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Vildagliptin 274901-16-5
| 产品描述 | |
| 描述 | Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions. |
| 纯度 | ＞98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 维达列汀；LAF237; NVP-LAF 237 |
| 外观 | 白色或类白色结晶性粉末 |
| 可溶性/溶解性 | DMSO : 56 mg/mL (184.6 mM) Ethanol : 56 mg/mL (184.6 mM) Water : 55 mg/mL (181.3 mM) |
| 生物活性 | |
| 靶点 | DPP-4 |
| In vitro(体外研究) | 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(体内研究) | 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. |
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| 研究领域 | |
| 研究领域 | CancerCancer MetabolismResponse to hypoxia Proteolysis / UbiquitinProteolytic enzymesSerine proteaseDPPs ImmunologyAdaptive ImmunityB CellsCD ImmunologyAdaptive ImmunityT CellsCD ImmunologyCell Type MarkersCDAdhesion ImmunologyCell Type MarkersCDNon-lineage ImmunologyImmune System DiseasesAntiviral SignalingHIV-related MetabolismPathways and ProcessesMetabolism processesHypoxia MicrobiologyOrganismVirusDNA VirusssRNA positive strand virusSARS Coronavirus Stem CellsHematopoietic ProgenitorsLymphoidB Lymphocytic Lineage Stem CellsHematopoietic ProgenitorsLymphoidT Lymphocytic Lineage Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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