ビルダグリプチン

化学名:ビルダグリプチン

CAS番号.274901-16-5

英語名:Vildagliptin

CBNumberCB71449010

MFC17H25N3O2

MW303.4

MOL File274901-16-5.mol

别名

ビルダグリプチン

ビルダグリプチン (JAN)

ビルダクリプチン

ビルダグリプチン物理性質

融点	153-155C
比旋光度	-78.3° (c = 9.73 in methanol)
沸点	531.3±50.0 °C(Predicted)
比重(密度)	1.27
闪点	275.1℃
貯蔵温度	Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解性	DMSO (最大 45mg/ml)、DMF (最大 20mg/ml) またはエタノール (最大 20mg/ml) に可溶。
外見	個体
酸解離定数(Pka)	15.05±0.40(Predicted)
色	白い
旋光度（Optical Rotation）	[α]/D -81 to -91°, c =0.1 in methanol
安定性：	購入日から2年間安定です。 DMSO、DMF、またはエタノールに溶解したこの溶液は、-20°C で 3 か月間保存できます。
InChI	InChI=1S/C17H25N3O2/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16/h12-14,19,22H,1-8,10-11H2/t12,13,14-,16,17/m0/s1
InChIKey	SYOKIDBDQMKNDQ-XWTIBIIYSA-N
SMILES	N1(C(CNC23CC4CC(CC(O)(C4)C2)C3)=O)CCC[C@H]1C#N
CAS データベース	274901-16-5(CAS DataBase Reference)

安全性情報

Rフレーズ	28-38-41-48
Sフレーズ	24/25-26-28-36/37/39
RIDADR	3077
WGK Germany	WGK 3
HSコード	29339900
ストレージクラス	11 - Combustible Solids

危険有害性情報のコード(GHS)

ビルダグリプチン化学特性,用途語,生産方法

効能
糖尿病治療薬, DPP-4阻害薬
商品名
エクア (ノバルティスファーマ)
説明
Vildagliptin, a DPP-4 inhibitor, was launched for the oral treatment of type 2 diabetes. Vildagliptin is the second DPP-4 inhibitor to reach the market behind sitagliptin, which was introduced in 2006. DPP-4 inhibitors act by slowing the inactivation of incretins, which are endogenous peptides involved in the physiologic regulation of glucose homeostasis. When blood glucose concentrations are normal or elevated, GLP-1 and GIP increase the synthesis and release of insulin from pancreatic βcells via intracellular signaling pathways involving cAMP. GLP-1 also lowers glucagon secretion from pancreatic α cells, which leads to reduced hepatic glucose production. However, although GLP-1 and GIP effectively lower blood glucose, they are short-lived as a result of rapid inactivation by the ubiquitous serine protease DPP-4. By inhibiting DPP-4, vildagliptin increases the concentration and duration of active incretin levels, which in turn results in increased insulin release and decreased glucagon levels in a glucose-dependent manner. Both vildagliptin and sitagliptin are potent, competitive, reversible inhibitors of DPP- 4 (IC₅₀=3.5 and 18 nM, respectively), and they both show slow, tight-binding inhibition kinetics.
化学的特性
White Solid
来歴
Vildagliptin is an oral anti-hyperglycemic agent (anti-diabetic drug) of the dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs.
It was approved by the European Medicines Agency (EMA) in 2007. The European Medicines Agency has also approved a combination of vildagliptin and metformin, vildagliptin/metformin (Eucreas by Novartis) as an oral treatment for type-2 diabetes.
使用
Labelled Vildagliptin. It is a new oral anti-hyperglycemic agent of a new dipeptidyl peptidase-IV (DPP-IV) inhibitor class of drugs. Antidiabetic.
副作用
The most common adverse events reported in patients receiving vildagliptin included headache, nasopharyngitis, cough, constipation, dizziness, and increased sweating. Vildagliptin is not recommended for patients with liver impairment.

ビルダグリプチン生産企業

ビルダグリプチンスペクトルデータ(¹HNMR)

274901-16-5, ビルダグリプチンキーワード

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ビルダグリプチン

危険有害性情報のコード(GHS)

ビルダグリプチン 化学特性,用途語,生産方法

ビルダグリプチン 生産企業

ビルダグリプチン スペクトルデータ(1HNMR)

274901-16-5, ビルダグリプチン キーワード

ビルダグリプチン化学特性,用途語,生産方法

ビルダグリプチン生産企業

ビルダグリプチンスペクトルデータ(¹HNMR)

274901-16-5, ビルダグリプチンキーワード