2. GPCR/G Protein Anti-infection Membrane Transporter/Ion Channel
  3. Adenosine Receptor HBV SGLT
  4. Swertisin

Swertisin is an oral adenosine A1 receptor antagonist and an SGLT2 inhibitor. Swertisin has anti-diabetic, antioxidant properties, inhibits HBV, and improves cognitive and memory impairments in mice.

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Swertisin Chemical Structure

Swertisin Chemical Structure

CAS No. : 6991-10-2

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Based on 1 publication(s) in Google Scholar

Other Forms of Swertisin:

Swertisin Related Antibodies

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1 Publications Citing Use of MCE Swertisin

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SGLT1 SGLT2

  • Biological Activity

  • Purity & Documentation

  • References

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Description

Swertisin is an oral adenosine A1 receptor antagonist and an SGLT2 inhibitor. Swertisin has anti-diabetic, antioxidant properties, inhibits HBV, and improves cognitive and memory impairments in mice[1][2][3].

IC50 & Target

SGLT2

 

In Vitro

Swertisin (7.5 μg/mL, 0-12 h) inhibits glucose uptake in HEK293 cells and reduces the expression of SGLT2[2].
Swertisin (0.2-5 μM, 6-12 days) suppresses levels of HBsAg, HBeAg and HBV DNA in HepG2.2.15 and HBV-infected HepG2-NTPC cells[3].

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

Swertisin Related Antibodies

Western Blot Analysis[2]

Cell Line: HEK293T
Concentration: 7.5 μg/mL
Incubation Time: 0, 4, 8, 12 h
Result: Decreased the expression of SGLT2 in a dose-dependent manner, while PKC expression was upregulated.

Real Time qPCR[3]

Cell Line: HepG2.2.15, HepG2-NTPC
Concentration: 0.2, 0.5, 1, 2, 5 μM
Incubation Time: 7 days; 6, 9, 12 days
Result: Reduced HBsAg and HBeAg levels.
In Vivo

Swertisin (30 mg/kg, orally, single dose) helps improve symptoms of schizophrenia in mice, including sensory motor gating disruptions and cognitive impairments[1].
Swertisin (2.5 mg/kg, intraperitoneally, once daily, days) reduces the expression of SGLT2 in mouse kidney tissue and can quickly lower blood sugar[2].
Swertisin (0-10 mg/kg, intraperitoneally, every other day, 20 days) significantly inhibits HBV replication in a HBV transgenic mouse model[3].

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

Animal Model: Mice induced by MK801 (HY-15084B)[1]
Dosage: 30 mg/kg; single dose
Administration: Oral gavage (p.o.)
Result: Alleviated the pre-pulse inhibition defect, reversed memory recognition impairment, and the elevated phosphorylation levels of Akt and GSK-3β signaling molecules in the prefrontal cortex restore normal function.
Animal Model: BALB/c mice induced by STZ (HY-13753)[2]
Dosage: 2.5 mg/kg; daily; 15 days
Administration: Intraperitoneal injection (i.p.)
Result: Improved overall glucose homeostasis, reduced SGLT2 expression in renal tissue, reduced PKC expression, and had a rapid hypoglycemic effect.
Animal Model: HBV transgenic mice[3]
Dosage: 0, 5, 10 mg/kg; every other day; 20 days
Administration: Intraperitoneal injection (i.p.)
Result: Showed that there was no significant weight loss, no significant changes in serum ALT and AST levels, and reduced serum HBsAg and HBeAg levels.
Molecular Weight

446.40

Formula

C22H22O10
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C=C(C2=CC=C(O)C=C2)OC3=CC(OC)=C([C@H]4[C@@H]([C@H]([C@@H]([C@@H](CO)O4)O)O)O)C(O)=C13
Structure Classification
Initial Source
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: 

DMSO : 50 mg/mL (112.01 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 2.2401 mL 11.2007 mL 22.4014 mL
5 mM 0.4480 mL 2.2401 mL 4.4803 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.

  • 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: ≥ 1.25 mg/mL (2.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: ≥ 1.25 mg/mL (2.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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 (protect from light)

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

Purity: 99.75%

SDS (251 KB)

COA (249 KB) HNMR (142 KB) CNMR (138 KB) RP-HPLC (150 KB) MS (137 KB)

Handling Instructions (2659 KB)
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 (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
DMSO 1 mM 2.2401 mL 11.2007 mL 22.4014 mL 56.0036 mL
5 mM 0.4480 mL 2.2401 mL 4.4803 mL 11.2007 mL
10 mM 0.2240 mL 1.1201 mL 2.2401 mL 5.6004 mL
15 mM 0.1493 mL 0.7467 mL 1.4934 mL 3.7336 mL
20 mM 0.1120 mL 0.5600 mL 1.1201 mL 2.8002 mL
25 mM 0.0896 mL 0.4480 mL 0.8961 mL 2.2401 mL
30 mM 0.0747 mL 0.3734 mL 0.7467 mL 1.8668 mL
40 mM 0.0560 mL 0.2800 mL 0.5600 mL 1.4001 mL
50 mM 0.0448 mL 0.2240 mL 0.4480 mL 1.1201 mL
60 mM 0.0373 mL 0.1867 mL 0.3734 mL 0.9334 mL
80 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.7000 mL
100 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5600 mL
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Swertisin 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:

Swertisin6991-10-2Adenosine ReceptorHBVSGLTP1 receptorHepatitis B virusSodium-dependent glucose cotransportersDiabetesanti-inflammatoryantioxidantHEK293TInhibitorinhibitorinhibit

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