| Bioactivity | 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]. |
| Invitro | Midaglizole stimulates insulin release with the EC50 values of 200 nM, 24 µM for rat islets and MIN6 β-cell line, respectively[3]. |
| In Vivo | 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: |
| Name | Midaglizole |
| CAS | 66529-17-7 |
| Formula | C16H17N3 |
| Molar Mass | 251.33 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |