2. Mizagliflozin

Mizagliflozin  (Synonyms: DSP-3235 free base; KGA-3235 free base; GSK-1614235 free base)

Cat. No.: HY-17638 Purity: 98.87%
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Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation.

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Mizagliflozin Chemical Structure

Mizagliflozin Chemical Structure

CAS No. : 666843-10-3

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10 mM * 1 mL in DMSO
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Based on 2 publication(s) in Google Scholar

Mizagliflozin Related Antibodies

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Description

Mizagliflozin (DSP-3235 free base) is a potent, orally active and selective SGLT1 inhibitor, with a Ki of 27 nM for human SGLT1. Mizagliflozin displays 303-fold selectivity over SGLT2. Mizagliflozin is used as an antidiabetic agent that can modify postprandial blood glucose excursion. Mizagliflozin also exhibits potential in the amelioration of chronic constipation[1].

IC50 & Target

Ki: 27 nM (hSGLT1), 8170 nM (hSGLT2)[1]
In Vivo

Mizagliflozin (DSP-3235 free base) (3-30 mg/kg; oral) exerts a laxative effect[1].
? Mizagliflozin administrated intravenously (0.3?mg/kg) and orally (3?mg/kg) declined with a short half-life (0.23 and 1.14?h, respectively)[2]

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

Animal Model: Male Wistar rats (rat model of low-fiber-diet-induced constipation)[1]
Dosage: 3, 10, 30 mg/kg
Administration: Oral
Result: Increased fecal wet weight in a rat model of low-fiber-diet-induced constipation.
Clinical Trial
Molecular Weight

564.67

Formula

C28H44N4O8
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(N)C(C)(C)CNCCCOC1=CC=C(CC2=C(C(C)C)NN=C2O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)C(C)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

H2O : ≥ 100 mg/mL (177.09 mM)

DMSO : 100 mg/mL (177.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7709 mL 8.8547 mL 17.7095 mL
5 mM 0.3542 mL 1.7709 mL 3.5419 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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: ≥ 2.5 mg/mL (4.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

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 (protect from light). 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
H2O / DMSO 1 mM 1.7709 mL 8.8547 mL 17.7095 mL 44.2736 mL
5 mM 0.3542 mL 1.7709 mL 3.5419 mL 8.8547 mL
10 mM 0.1771 mL 0.8855 mL 1.7709 mL 4.4274 mL
15 mM 0.1181 mL 0.5903 mL 1.1806 mL 2.9516 mL
20 mM 0.0885 mL 0.4427 mL 0.8855 mL 2.2137 mL
25 mM 0.0708 mL 0.3542 mL 0.7084 mL 1.7709 mL
30 mM 0.0590 mL 0.2952 mL 0.5903 mL 1.4758 mL
40 mM 0.0443 mL 0.2214 mL 0.4427 mL 1.1068 mL
50 mM 0.0354 mL 0.1771 mL 0.3542 mL 0.8855 mL
60 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7379 mL
80 mM 0.0221 mL 0.1107 mL 0.2214 mL 0.5534 mL
100 mM 0.0177 mL 0.0885 mL 0.1771 mL 0.4427 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

Keywords:

Mizagliflozin666843-10-3DSP-3235KGA-3235GSK-1614235DSP3235DSP 3235KGA3235KGA 3235GSK1614235GSK 1614235Inhibitorinhibitorinhibit

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