Midaglizole hydrochloride

Research use only, not for human use.

Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferred α2-adrenoceptor antagonist. Midazolazole hydrochloride (DG5128) has an affinity for α2-adrenoceptor (pKi = 6.28) 7.4 times higher than that of α1-adrenoceptor.

Midaglizole hydrochloride (DG5128) is a preferential α2-adrenoceptor antagonist. Midaglizole hydrochloride (DG5128) exhibits 7.4 times higher affinity (pKi=6.28) toward α2-adrenoceptor than α1-adrenoceptor.

Midaglizole (DG-5128) at concentrations up to 10 μM inhibits [3H]clonidine binding more effectively than it doed [3H]prazosin binding in rat cerebral cortex membranes. The mode of inhibition is homogeneous and consistent with the law of simple mass action. The EC50 values for stimulation of insulin release from rat islets and the MIN6 β-cell line induced by Midaglizole are 200 nM and 24 μM, respectively. The IC50 values for KATP current inhibition induced by Midaglizole are 3.8 μM and 4.4 uM for Kir6.2 and Kir6.2/SUR1 , respectively.

Midaglizole (3 and 30 mg/kg, i.v.) increases blood pressure in pithed rats.

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GPCR/G Protein

Adrenergic Receptor

Adrenergic Receptor

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79689-25-1

324.25

C16H19Cl2N3

>98% (HPLC)

In Vitro:?DMSO : 500 mg/mL (1542.02 mM; Ultrasonic (<60°C)

C1(C(CC2=NCCN2)C3=CC=CC=C3)=NC=CC=C1.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years