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    Gliquidone (AR-DF26)
    Gliquidone (AR-DF26)

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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 #: V0218
    CAS #: 33342-05-1 Purity ≥98%

    Description: Gliquidone  (also known as AR-DF 26; Glurenorm; Beglynor) is a potent ATP-sensitive K+ channel antagonist with potential anti0diabetic activity. It inhibits ATP-sensitive K + channel with an IC50 of 27.2 NM. As a sulfonylurea anti-diabetic drug , it is used in the treatment of diabetes mellitus type 2. In patients with type 2 diabetes mellitus, gliquidone reduced the mean plasma glucose levels by 15% and increased insulin levels by 40%. In Caucasian patients with new-onset diabetes mellitus (NODM) after kidney transplantation, gliquidone reduced fasting blood glucose (FBG) from 154 mg/dl to 120 mg/dl.

    References: Fundam Clin Pharmacol. 1991;5(2):107-15; Arzneimittelforschung. 1997 Mar;47(3):247-52.

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    Molecular Weight (MW)527.63 
    FormulaC27H33N3O6S 
    CAS No.33342-05-1 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 105 mg/mL (199.0 mM) 
    Water: <1 mg/mL
    Ethanol: 6 mg/mL (11.4 mM) 
    Solubility (In vivo)2% DMSO+Corn oil: 5mg/mL  
    Synonyms

    Synonym: Gliquidone; Glurenorm; Beglynor; Glikvidon; Glycvidon; Sanofi Synthelabo brand of gliquidone; Yamanouchi brand of gliquidone; AR-DF 26

    IUPAC/Chemical Name: 1-cyclohexyl-3-[4-[2-(7-methoxy-4,4-dimethyl-1,3-dioxoisoquinolin-2-yl)ethyl]phenyl]sulfonylurea

    InChi Key: LLJFMFZYVVLQKT-UHFFFAOYSA-N

    InChi Code: InChI=1S/C27H33N3O6S/c1-27(2)23-14-11-20(36-3)17-22(23)24(31)30(25(27)32)16-15-18-9-12-21(13-10-18)37(34,35)29-26(33)28-19-7-5-4-6-8-19/h9-14,17,19H,4-8,15-16H2,1-3H3,(H2,28,29,33)

    SMILES Code: CC1(C2=C(C=C(C=C2)OC)C(=O)N(C1=O)CCC3=CC=C(C=C3)S(=O)(=O)NC(=O)NC4CCCCC4)C


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    In Vitro

    In vitro activity: Gliquidone is an ATP-sensitive K+ channel antagonist. In mice, gliquidone (10 or 40 μg) antagonized morphine (20 mg/kg) induced hypermotility in a dose-dependent way. These results suggested that ATP-sensitive K+ channels played an important role in morphine-induced hypermotility.

    In VivoGliquidone (0.1–1.0 μg per mouse i.c.v.) prevents antinociception produced by amitriptyline and clomipramine in a dose-dependent manner in male swiss albino mice. Gliquidone (0.06–16 μg per mouse, i.c.v.) antagonizes the antinociception induced by buprenorphine, morphine and methadone. Gliquidone (6 μg per mouse, i.c.v.) prevents the antinociception induced by clonidine (0.125 mg/kg, s.c.) and guanabenz (0.30 mg/kg, s.c.), while a lower dose of gliquidone (3 μg per mouse, i.c.v.) is ineffective. Glurenorm (10 mg/kg) given to the diabetic rats produces significant reductions in blood glucose, nonenzymatic glycosylation, and total protein in the lenses, and significantly increases in glutathione levels in the lenses. 
    Animal modelMice
    Formulation & Dosage10 mg/kg
    References

    Fundam Clin Pharmacol. 1991;5(2):107-15; Neuropharmacology. 2001;40(1):75-84; Br J Pharmacol. 1995 Mar;114(6):1296-302. 


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

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