Midaglizole
Based on 1 Customer Validation
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.
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- Pureté : 98.28%
- CAS No.: 66529-17-7
- Formule: C16H17N3
- Masse moléculaire:251.33
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
In Vivo
Midaglizole (0.2, 1, 2 mg/kg; infusion) reduces blood glucose levels in dags[2].
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 No. 66529-17-7
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Appearance Solid
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Masse moléculaire 251.33
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Formule C16H17N3
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Color White to off-white
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SMILES
C1(C(C2=CC=CC=C2)CC3=NCCN3)=NC=CC=C1
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Synonyms
(±)-DG5128 free base; DG5128 free base
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
DMSO : 162.5 mg/mL (646.56 mM; Need ultrasonic; 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 16.25 mg/mL (64.66 mM); Clear solution
This protocol yields a clear solution of ≥ 16.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (162.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 16.25 mg/mL (64.66 mM); Clear solution
This protocol yields a clear solution of ≥ 16.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (162.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (277 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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Instruction de manipulation (2659 KB)
Références
[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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.9788 mL | 19.8942 mL | 39.7883 mL | 99.4708 mL |
| 5 mM | 0.7958 mL | 3.9788 mL | 7.9577 mL | 19.8942 mL | |
| 10 mM | 0.3979 mL | 1.9894 mL | 3.9788 mL | 9.9471 mL | |
| 15 mM | 0.2653 mL | 1.3263 mL | 2.6526 mL | 6.6314 mL | |
| 20 mM | 0.1989 mL | 0.9947 mL | 1.9894 mL | 4.9735 mL | |
| 25 mM | 0.1592 mL | 0.7958 mL | 1.5915 mL | 3.9788 mL | |
| 30 mM | 0.1326 mL | 0.6631 mL | 1.3263 mL | 3.3157 mL | |
| 40 mM | 0.0995 mL | 0.4974 mL | 0.9947 mL | 2.4868 mL | |
| 50 mM | 0.0796 mL | 0.3979 mL | 0.7958 mL | 1.9894 mL | |
| 60 mM | 0.0663 mL | 0.3316 mL | 0.6631 mL | 1.6578 mL | |
| 80 mM | 0.0497 mL | 0.2487 mL | 0.4974 mL | 1.2434 mL | |
| 100 mM | 0.0398 mL | 0.1989 mL | 0.3979 mL | 0.9947 mL |
Midaglizole Related Classifications
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