Midaglizole hydrochloride
Based on 1 Customer Validation
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.
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- Reinheit: 99.90%
- CAS. Nr.: 79689-25-1
- Formel: C16H19Cl2N3
- Molecular Weight:324.25
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
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α adrenergic receptor |
In Vitro
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:290-450 g, Male Wistar rats[1]
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Dosage:3, 30 mg/kg
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Administration:I.v
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Result:Increased the blood pressure by 27 and 64 mmHg at 3, 30 mg/kg, respectively.
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Animal Model:Dogs[2]
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Dosage:0.2, 1, 2 mg/kg
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Administration:Superior pancreaticoduodeneal artery infusion
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Result:Reduced blood glucose levels by stimulating insulin release from the pancreatic islets.
Chemical Information
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CAS. Nr. 79689-25-1
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Appearance Solid
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Molecular Weight 324.25
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Formel C16H19Cl2N3
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Color White to off-white
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SMILES
C(C1=CC=CC=C1)(C2=CC=CC=N2)CC3=NCCN3.Cl
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Synonyms
(±)-DG5128; DG5128
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 500 mg/mL (1542.02 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[2]. Ohneda K, et al. Mechanism of insulin secretion by midaglizole. Diabetes Res Clin Pract. 1993 Feb;19(2):127-32. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.0840 mL | 15.4202 mL | 30.8404 mL | 77.1010 mL |
| 5 mM | 0.6168 mL | 3.0840 mL | 6.1681 mL | 15.4202 mL | |
| 10 mM | 0.3084 mL | 1.5420 mL | 3.0840 mL | 7.7101 mL | |
| 15 mM | 0.2056 mL | 1.0280 mL | 2.0560 mL | 5.1401 mL | |
| 20 mM | 0.1542 mL | 0.7710 mL | 1.5420 mL | 3.8551 mL | |
| 25 mM | 0.1234 mL | 0.6168 mL | 1.2336 mL | 3.0840 mL | |
| 30 mM | 0.1028 mL | 0.5140 mL | 1.0280 mL | 2.5700 mL | |
| 40 mM | 0.0771 mL | 0.3855 mL | 0.7710 mL | 1.9275 mL | |
| 50 mM | 0.0617 mL | 0.3084 mL | 0.6168 mL | 1.5420 mL | |
| 60 mM | 0.0514 mL | 0.2570 mL | 0.5140 mL | 1.2850 mL | |
| 80 mM | 0.0386 mL | 0.1928 mL | 0.3855 mL | 0.9638 mL | |
| 100 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7710 mL |
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