Repaglinide - Moligand™, 10mM in DMSO , Sulfonylurea receptor 1, Kir6.2 blocker, CAS No.135062-02-1, Sulfonylurea receptor 1, Kir6.2 blocker

CAS: 135062-02-1 Cat. No.: R408416 分子式: C₂₇H₃₆N₂O₄ 分子量: 452.59 EC番号: 629-921-1 PubChem CID: 65981

グレード＆純度 Moligand™, 10mM in DMSO

Synonyms

AG-EE 623 ZW | (S)-2-ethoxy-4-(2-(3-methyl-1-(2-(piperidin-1-yl)phenyl)butylamino)-2-oxoethyl)benzoic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Information

Repaglinide Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.
In vitro

Repaglinide is found to bind with low affinity (K(D)=59 nM) to SUR1 alone, but with high affinity (increased approximately 150-fold) when SUR1 is co-expressed with Kir6.2. Repaglinide binds with low affinity (K(D)=51 nM) to SUR1 co-expressed with Kir6.2DeltaN14. Repaglinide lowers the plasma glucose concentration in the control rat, whilst failing to affect significantly the plasma insulin concentration or insulin/glucose ratio. Repaglinide administration affects neither plasma glucose nor insulin concentration, restores a normal value for the otherwise abnormally high basal insulin output, increases the 16.7 mM/2.8 mM ratio for insulin release, and again augmented protein biosynthesis at both low and high hexose concentrations in Goto-Kakizaki (GK) rats. Repaglinide is found to bind to NCS proteins, but not to CaM or S100 proteins, in a Ca2+-dependent manner. Repaglinide antagonizes the inhibitory action of recoverin in a rhodopsin kinase assay with IC50 values of 400 mM. Repaglinide tightly binds to the visinin-like domain of CCaMK and PpCaMK in a Ca2+-dependent manner and antagonizes the regulatory function of the domain with IC50 values of 55 and 4 mM for CCaMK and PpCaMK respectively.

In vivo

Repaglinide provokes a greater and more rapid increase in plasma insulin concentration and an earlier fall in glycemia than those observed after administration of the hypoglycemic sulfonylureas in both fed and starved normal rats.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

仕様

同義語

AG-EE 623 ZW | (S)-2-ethoxy-4-(2-(3-methyl-1-(2-(piperidin-1-yl)phenyl)butylamino)-2-oxoethyl)benzoic acid

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

BLOCKER, INHIBITOR

作用メカニズム

Sulfonylurea receptor 1, Kir6.2 blocker

製品の性質

ALogP

5.2

名前と識別子

異性体SMILES

CCOC1=C(C=CC(=C1)CC(=O)N[C@@H](CC(C)C)C2=CC=CC=C2N3CCCCC3)C(=O)O

WGKドイツ

2

RTECS

DI0876305

PubChem CID

65981

分子量

452.59

関連ターゲット（人間）

ABCC8 Tclin ATP-binding cassette sub-family C member 8 (3 Activities)

Discover Target: ABCC8

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

化学的性質と物理的性質

• 比旋光度［α］: 9° (C=1,MeOH)
• 融点（°C）: 133 °C