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 Fórmula: C₂₇H₃₆N₂O₄ Peso molecular: 452.59 Número EC: 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

Descripción general

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

Sinónimos

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

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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.

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

BLOCKER, INHIBITOR

Mecanismo de acción

Sulfonylurea receptor 1, Kir6.2 blocker

Propiedades del producto

• ALogP: 5.2

Nombres e identificadores

• Isómeros SMILES: CCOC1=C(C=CC(=C1)CC(=O)N[C@@H](CC(C)C)C2=CC=CC=C2N3CCCCC3)C(=O)O
• WGK Alemania: 2
• RTECS: DI0876305
• PubChem CID: 65981
• Peso molecular: 452.59

Objetivos asociados (humanos)

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)

Propiedades químicas y físicas

• Rotación específica [α]: 9° (C=1,MeOH)
• Punto de fusión (°C): 133 °C

Referencias

1. Zixian He, Zhiwei Liu, Haihuan Xie, Pengjie Luo, Xiangmei Li.  (2023)  An Ultrasensitive Lateral Flow Immunoassay Based on Metal-Organic Framework-Decorated Polydopamine for Multiple Sulfonylureas Adulteration in Functional Foods.  Foods,  12  (3): (539).  [PMID:36766067] [10.3390/foods12030539]

2. Haihuan Xie, Yingying Li, Jin Wang, Yi Lei, Anastasios Koidis, Xiangmei Li, Xing Shen, Zhenlin Xu, Hongtao Lei.  (2021)  Broad-specific immunochromatography for simultaneous detection of various sulfonylureas in adulterated multi-herbal tea.  FOOD CHEMISTRY,      [PMID:34536782] [10.1016/j.foodchem.2021.131055]

3. Xiaoming Zou, Baoyin Zhang, Yujiao Jing, Lihui Zong, Ligui Wu, Qunyan Zhou, Yue Fang, Kaifang Shen, Xubiao Luo, Lingling Rong.  (2025)  Significant effects of electrophilicity in oral antidiabetic drugs upon conjugative transfer of drug-resistance plasmids in activated sludge and the mechanisms.  WATER RESEARCH,      [PMID:41442951] [10.1016/j.watres.2025.125250]