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    Glyburide (Glibenclamide)
    Glyburide (Glibenclamide)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1678
    CAS #: 10238-21-8Purity ≥98%

    Description: Glyburide (formerly HB419; HB420; Glibenclamide; Micronase; Diabeta; Maninil; Micronase; Neogluconin) is a selective blocker of vascular ATP-sensitive K+ channels (KATP) that has been approved as an antidiabetic sulfonylurea drug used for the treatment of type 2 diabetes. Its actions are similar to those of chlorpropamide that can potentially be used to decrease cerebral edema.

    References: J Pharmacol Exp Ther. 1989 Jan;248(1):149-56; J Pharmacol Exp Ther. 1993 May;265(2):933-7.

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    Molecular Weight (MW)494
    FormulaC23H28ClN3O5S
    CAS No.10238-21-8
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 99 mg/mL (200.4 mM)
    Water:<1 mg/mL
    Ethanol:<1 mg/mL
    Other info

    Chemical Name: 5-chloro-N-[2-[4-(cyclohexylcarbamoylsulfamoyl)phenyl]ethyl]-2-methoxybenzamide

    InChi Key: ZNNLBTZKUZBEKO-UHFFFAOYSA-N

    InChi Code: InChI=1S/C23H28ClN3O5S/c1-32-21-12-9-17(24)15-20(21)22(28)25-14-13-16-7-10-19(11-8-16)33(30,31)27-23(29)26-18-5-3-2-4-6-18/h7-12,15,18H,2-6,13-14H2,1H3,(H,25,28)(H2,26,27,29)

    SMILES Code: COC1=C(C=C(C=C1)Cl)C(=O)NCCC2=CC=C(C=C2)S(=O)(=O)NC(=O)NC3CCCCC3

    Synonyms

    HB-420; Glyburide; Glibenclamide; HB419; HB420; Micronase; Diabeta; Maninil; Micronase; Neogluconin


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    In Vitro

    In vitro activity: 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 VivoGlyburide (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.
    Animal modelRats
    Formulation & Dosage25 mg/kg i.v.
    References

    J Pharmacol Exp Ther. 1989 Jan;248(1):149-56; J Pharmacol Exp Ther. 1993 May;265(2):933-7.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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