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Rosiglitazone maleate

Rosiglitazone maleate 구조식 이미지
카스 번호:
155141-29-0
상품명:
Rosiglitazone maleate
동의어(영문):
Avandi;BRL-49653c;RSIGLITAZONEMALEATE;RosiglitazoneTartrate;ROSIGLITAZONE MALEATE;Rosiglitazone-d3 Maleate;Rosiglitazone Maleate forM;Rosiglitazone Maleate (200 mg);Rosiglitazone maleate Solution, 1000ppm;5-{p-[2-(methyl-2-pyridylamino)ethoxy]benzyl}-2,4-thiazolidinedione maleate
CBNumber:
CB0133276
분자식:
C22H23N3O7S
포뮬러 무게:
473.5
MOL 파일:
155141-29-0.mol

Rosiglitazone maleate 속성

녹는점
235-240°C
저장 조건
-20°C Freezer
산도 계수 (pKa)
6.1; 6.8(at 25℃)
물리적 상태
White powder
CAS 데이터베이스
155141-29-0(CAS DataBase Reference)

안전

위험품 표기 Xi
위험 카페고리 넘버 20/21/22-36/38
안전지침서 24/25-37/39-26
WGK 독일 3

Rosiglitazone maleate C화학적 특성, 용도, 생산

개요

Rosiglitazone maleate, belongs to a novel class of thiazolidine diones launched for the treatment of non-insulin-dependent diabetes mellitus (NIDDM), a disease characterized by a pancreatic β-cell defect and insulin resistance in the liver and peripheral tissues. The racemic base can be obtained by KnSvenagel condensation between 2, 4-thiazolidinedione and the corresponding 4-substituted benzaldehyde (itself prepared in 2 steps from 2-chloropyridine), followed by reduction of the benzylidene. Rosiglitazone was shown to be a potent agonist of peroxisome proliferator activated receptor-gamma (PPARgamma), a nuclear receptor involved in the differentiation of adipose tissue, without activating liver PPAR-alpha receptors. This activation of PPAR-gamma could mediate the down-regulation of leptin gene expression. In animal models, Rosiglitazone has been shown to normalize glucose metabolism and reduce the exogenous dose of insulin needed to achieve glycemic control. In patients with Type II diabetes, daily doses (4 or 8 mg) of Rosiglitazone significantly improved blood sugar control without affecting cardiac structure or function.

화학적 성질

White To Off-White Solid

Originator

SmithKline Beecham (US)

용도

Insulin sensitizer; binds to peroxisome proliferator activated receptor gamma (PPAR- γ).

용도

Thiazole alkanes antidiabetic drug

용도

Thiazolidinediones (TZDs) are a group of structurally related peroxisome proliferator-activated receptor γ (PPARγ) agonists with antidiabetic actions in vivo. Rosiglitazone is a prototypical TZD that has served as a reference compound for this class. It is a potent and selective PPARγ ligand that binds to the PPARγ ligand-binding domain with a Kd value of 43 nM. It activates luciferase-based expression constructs PPARγ1 and PPARγ2 with EC50 values of approximately 30 nM and 100 nM, respectively. Rosiglitazone is active in vivo as an antidiabetic agent in the ob/ob mouse model, and has been used as an oral hypoglycemic agent in the treatment of type 2 diabetes in humans for many years.[Cayman Chemical]

상표명

Avandia (GlaxoSmithKline).

Rosiglitazone maleate 준비 용품 및 원자재

원자재

준비 용품


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