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 Formula: C₂₇H₃₆N₂O₄ Molecular Weight: 452.59 EC Number: 629-921-1 PubChem CID: 65981

GRADE & PURITY 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

Overview

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%

Specifications

Synonyms

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

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

BLOCKER, INHIBITOR

Mechanism of action

Sulfonylurea receptor 1, Kir6.2 blocker

Product Properties

ALogP

5.2

Names and Identifiers

Isomeric SMILES

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

WGK Germany

2

RTECS

DI0876305

PubChem CID

65981

Molecular Weight

452.59

Associated Targets(Human)

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)

Chemical and Physical Properties

• Specific Rotation[α]: 9° (C=1,MeOH)
• Melt Point(°C): 133 °C