Midaglizole hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Midaglizole hydrochloride (DG5128)是有效的 α2-肾上腺素受体拮抗剂。Midaglizole hydrochloride (DG5128)对 α2-肾上腺素能受体的亲和力 (pKi= 6.28) 比 α1-肾上腺素能受体高 7.4 倍。

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.

——

GPCR/G Protein

Adrenergic Receptor

Adrenergic Receptor

——

——

79689-25-1

324.25

C16H19Cl2N3

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 500 mg/mL (1542.02 mM; 超声助溶 (<60°C)

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

——

(-20℃)

With Ice Pack

≥ 2 years