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Midaglizole

(Synonyms: (±)-DG5128 free base; DG5128 free base) 目录号 : GC67691

Midaglizole ((±)-DG5128 free base, DG5128 free base) 是一种有效的 α2-adrenoceptor 拮抗剂。Midaglizole 是一种降血糖药。Midaglizole 在具有升高血压并降低血糖水平的作用。

Midaglizole Chemical Structure

Cas No.:66529-17-7

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10mg
¥6,120.00
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25mg
¥12,150.00
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Sample solution is provided at 25 µL, 10mM.

Description

Midaglizole ((±)-DG5128 free base, DG5128 free base) is a potent α2-adrenoceptor antagonist. Midaglizole is a hypoglycemic agent. Midaglizole increases blood pressure and reduces blood glucose levels in vivo[1][2][3].

Midaglizole stimulates insulin release with the EC50 values of 200 nM, 24 µM for rat islets and MIN6 β-cell line, respectively[3].

Midaglizole (3, 30 mg/kg; i.v.) increases blood pressure in rats[1].
Midaglizole (0.2, 1, 2 mg/kg; infusion) reduces blood glucose levels in dags[2].

Animal Model: 290-450 g, Male Wistar rats[1]
Dosage: 3, 30 mg/kg
Administration: I.v.
Result: Increased the blood pressure by 27 and 64 mmHg at 3, 30 mg/kg, respectively.
Animal Model: Dogs[2]
Dosage: 0.2, 1, 2 mg/kg
Administration: Superior pancreaticoduodeneal artery infusion
Result: Reduced blood glucose levels by stimulating insulin release from the pancreatic islets.

[1]. Hirohashi M, et al. Intrinsic pressor activity of midaglizole, an alpha-2 adrenoceptor antagonist, in pithed rats. Jpn J Pharmacol. 1990 Aug;53(4):519-20.
[2]. Ohneda K, et al. Mechanism of insulin secretion by midaglizole. Diabetes Res Clin Pract. 1993 Feb;19(2):127-32.
[3]. Proks P, et al. Inhibition of recombinant K(ATP) channels by the antidiabetic agents midaglizole, LY397364 and LY389382. Eur J Pharmacol. 2002 Sep 27;452(1):11-9.

化学性质

Cas No. 66529-17-7 SDF Download SDF
别名 (±)-DG5128 free base; DG5128 free base
分子式 C16H17N3 分子量 251.33
溶解度 DMSO : 162.5 mg/mL (646.56 mM; Need ultrasonic) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 3.9788 mL 19.8942 mL 39.7883 mL
5 mM 0.7958 mL 3.9788 mL 7.9577 mL
10 mM 0.3979 mL 1.9894 mL 3.9788 mL
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