2. Membrane Transporter/Ion Channel
  3. SGLT
  4. Henagliflozin

Henagliflozin (SHR3824) is a potent selective sodium-glucose co-transporter 2 (SGLT2) inhibitor with the IC50 values of 2.38 and 4324 nM for human SGLT2 and SGLT1, respectively. Henagliflozin can be used in diabetes research.

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Henagliflozin

Henagliflozin Chemical Structure

CAS No. : 1623804-44-3

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Based on 1 publication(s) in Google Scholar

Henagliflozin Related Antibodies

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Description

Henagliflozin (SHR3824) is a potent selective sodium-glucose co-transporter 2 (SGLT2) inhibitor with the IC50 values of 2.38 and 4324 nM for human SGLT2 and SGLT1, respectively. Henagliflozin can be used in diabetes research[1].

IC50 & Target

SGLT2

 

In Vivo

Henagliflozin (SHR3824) (p.o., 0.1-3.0 mg/kg, once) improves glucose tolerance in a dose-dependent manner in normal mice after exposure to glucose challenge[1].
Henagliflozin (SHR3824) (p.o., 0.3-3.0 mg/kg, once daily, 41 days) increases urinary glucose excretion in a dose-dependent manner and significantly reduces blood glucose levels in GK rats, with no effect on body weight or food intake. The HbA1c values of GK rats treated with 0.3, 1.0 or 3.0 mg/kg are 5.47%, 5.19% and 5.04%, respectively[1].
Henagliflozin (SHR3824) (p.o., 0.3-3.0 mg/kg, once daily, 43 days) causes a dose-dependent increase in urinary output and urinary glucose excretion in db/db mice, with a concomitant decrease in plasma glucose levels and no effect on body weight or food intake. The doses of 0.3, 1.0 or 3.0 mg/kg results in significant reductions in non-fasting and fasting glucose levels of 24.7%, 28.2% or 35.1% and 49.5%, 57.8% or 62.9%, respectively[1].

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

454.87

Formula

C22H24ClFO7
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@@]2(C3=CC(CC4=CC(F)=C(C=C4)OCC)=C(C=C3)Cl)O[C@](CO2)([C@H]([C@@H]1O)O)CO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.84 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 2.1984 mL 10.9922 mL 21.9843 mL
5 mM 0.4397 mL 2.1984 mL 4.3969 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. 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: ≥ 2.5 mg/mL (5.50 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 (5.50 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.
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).
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. 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 2.1984 mL 10.9922 mL 21.9843 mL 54.9608 mL
5 mM 0.4397 mL 2.1984 mL 4.3969 mL 10.9922 mL
10 mM 0.2198 mL 1.0992 mL 2.1984 mL 5.4961 mL
15 mM 0.1466 mL 0.7328 mL 1.4656 mL 3.6641 mL
20 mM 0.1099 mL 0.5496 mL 1.0992 mL 2.7480 mL
25 mM 0.0879 mL 0.4397 mL 0.8794 mL 2.1984 mL
30 mM 0.0733 mL 0.3664 mL 0.7328 mL 1.8320 mL
40 mM 0.0550 mL 0.2748 mL 0.5496 mL 1.3740 mL
50 mM 0.0440 mL 0.2198 mL 0.4397 mL 1.0992 mL
60 mM 0.0366 mL 0.1832 mL 0.3664 mL 0.9160 mL
80 mM 0.0275 mL 0.1374 mL 0.2748 mL 0.6870 mL
100 mM 0.0220 mL 0.1099 mL 0.2198 mL 0.5496 mL
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Henagliflozin Related Classifications

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:

Henagliflozin1623804-44-3SHR3824SHR 3824SHR-3824SGLTSodium-dependent glucose cotransportersSGLT2SGLT1diabetes researchInhibitorinhibitorinhibit

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