Midaglizole hydrochloride ((±)-DG5128) (Synonyms: (±)-DG5128; DG5128) |
| Catalog No.GC31615 |
Midaglizole hydrochloride ((±)-DG5128) (DG5128) is a preferential α2-adrenoceptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 79689-25-1
Sample solution is provided at 25 µL, 10mM.
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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[1]. 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[2].
Midaglizole (3 and 30 mg/kg, i.v.) increases blood pressure in pithed rats[3].
[1]. Yamanaka K, et al. The selectivity of DG-5128 as an alpha 2-adrenoceptor antagonist. Eur J Pharmacol. 1984 Nov 27;106(3):625-8. [2]. 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. [3]. 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.
Animal experiment: | Rats[3]Male Wistar rats (290-450 g) are anesthetized with pentobarbital sodium (35 mg/kg, i.p.) and artificially ventilated with room air. Diastolic blood pressure before the administration of the Midaglizole (Midaglizole) is about 35 mmHg. Midaglizole at doses of 3 and 30 mg/kg produces an increase in blood pressure by 27 and 64 mmHg, respectively, at approximately 1 min after the administration. |
References: [1]. Yamanaka K, et al. The selectivity of DG-5128 as an alpha 2-adrenoceptor antagonist. Eur J Pharmacol. 1984 Nov 27;106(3):625-8. | |
| Cas No. | 79689-25-1 | SDF | |
| Synonyms | (±)-DG5128; DG5128 | ||
| Canonical SMILES | C(C1=CC=CC=C1)(C2=CC=CC=N2)CC3=NCCN3.[2 HCl] | ||
| Formula | C16H19Cl2N3 | M.Wt | 324.25 |
| Solubility | DMSO : 500 mg/mL (1542.02 mM; ultrasonic and warming and heat to 60°C) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.084 mL | 15.4202 mL | 30.8404 mL |
| 5 mM | 616.8 μL | 3.084 mL | 6.1681 mL |
| 10 mM | 308.4 μL | 1.542 mL | 3.084 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
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