Glyburide (Glibenclamide) - Moligand™, 10mM in DMSO , Sulfonylurea receptor 1, Kir6.2 blocker, CAS No.10238-21-8, Sulfonylurea receptor 1, Kir6.2 blocker

CAS: 10238-21-8 Cat. No.: G407851 Peso molecular: 494.00 Número EC: 233-570-6

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

5-​chloro-​N-​[2-​[4-​[[[(cyclohexylamino)​carbonyl]​amino]​sulfonyl]​phenyl]​ethyl]​-​2-​methoxy-benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Glyburide (Glibenclamide) Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 diabetes.
In vitro

Glyburide (0.03 mM), a sulfonylurea which has been shown to block the ATP-modulated potassium channel in insulin-secreting cells, causes concentration-dependent shifts to the right (up to 100-fold) of the IC50 value for BRL 34915 and diazoxide, and at 1 μM, abolishes the relaxation response to minoxidil sulfate. Glyburide increases the apparent affinity of HDL binding to Scavenger receptor class B type I (SR-BI). Glyburide blocks SR-BI-mediated selective lipid uptake and efflux at a potency similar to that for its inhibition of ABCA1 (IC50 approximately 275-300 mM). Glyburide (6 mM) which reduces the opening of KATP channels, aggravates Ca2+ loading only when applied to dinitrophenol-pretreated myocytes but not when applied with dinitrophenol treatment. Glyburide (10-500 nM) produces a dose-dependent inhibition of the potassium channel openers (PCOs) relaxation time course. Glyburide also reverses existing Pinacidil relaxation regardless of the degree of pre-existing relaxation. Glyburideis is able to produce its blockade regardless of the state of K+ channel activation.

In vivo

Glyburide (GLY) dose-dependently increases urinary Na⁺ excretion with little change in urinary K+ excretion after i.p. administration (10-100 mg/kg) in saline-loaded conscious rats. Glyburide (25 mg/kg i.v.) increases Na⁺ excretion 350% during the first hour post-treatment without affecting K+ excretion, glomerular filtration rate, mean arterial pressure or heart rate.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

5-​chloro-​N-​[2-​[4-​[[[(cyclohexylamino)​carbonyl]​amino]​sulfonyl]​phenyl]​ethyl]​-​2-​methoxy-benzamide

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Glyburide (Glibenclamide) is a known blocker of vascular ATP-sensitive K+ channels (KATP), used in the treatment of type 2 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, CHANNEL BLOCKER, INHIBITOR

Mecanismo de acción

Sulfonylurea receptor 1, Kir6.2 blocker

Propiedades del producto

• ALogP: 4.8

Nombres e identificadores

• Isómeros SMILES: COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3
• WGK Alemania: 2
• RTECS: YS4725200
• Peso molecular: 494.00
• Reaxy-Rn: 2230085
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=2230085&ln=

Objetivos asociados (humanos)

CFTR Tclin Cystic fibrosis transmembrane conductance regulator (1 Activities)

Discover Target: CFTR

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

KCNJ11 Tclin ATP-sensitive inward rectifier potassium channel 11 (1 Activities)

Discover Target: KCNJ11

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

Propiedades químicas y físicas

• Índice de refracción: 1.62
• Punto de fusión (°C): 171-174°C

Referencias

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8. Qiao-Lai Wang, Pei-Xi Zhang, Rui Shen, Meng Xu, Liang Han, Xuan Shi, Zi-Rui Zhou, Jing-Yi Yang, Jie-Qing Liu.  (2024)  Determination of arbutin in vitro and in vivo by LC-MS/MS: Pre-clinical evaluation of natural product arbutin for its early medicinal properties.  JOURNAL OF ETHNOPHARMACOLOGY,      [PMID:38670407] [10.1016/j.jep.2024.118232]

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