1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. Midaglizole

Midaglizole  (Synonyms: (±)-DG5128 free base; DG5128 free base)

Cat. No.: HY-148529 Purity: 98.28%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Midaglizole Chemical Structure

Midaglizole Chemical Structure

CAS No. : 66529-17-7

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1 mg USD 160 In-stock
5 mg USD 400 In-stock
10 mg USD 680 In-stock
25 mg USD 1350 In-stock
50 mg USD 2200 In-stock
100 mg USD 3400 In-stock
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Based on 1 publication(s) in Google Scholar

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  • References

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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].

In Vitro

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

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

251.33

Formula

C16H17N3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C1(C(C2=CC=CC=C2)CC3=NCCN3)=NC=CC=C1

Shipping

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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Midaglizole
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