1. Immunology/Inflammation NF-κB Apoptosis Epigenetics PI3K/Akt/mTOR
  2. Toll-like Receptor (TLR) NF-κB TNF Receptor AMPK
  3. Kaempferol 3-O-sophoroside

Kaempferol 3-O-sophoroside is an orally active derivative of Kaempferol. It exhibits anti-inflammatory, analgesic, and antidepressant effects. Kaempferol 3-O-sophoroside is an inhibitor of the cell surface receptor toll-like receptor (TLR) 2/4 for High mobility group box 1 (HMGB1), and it also exerts anti-inflammatory effects by blocking the activation of NF-κB expression and the production of TNF-α. Kaempferol 3-O-sophoroside promotes the production of brain-derived neurotrophic factor (BDNF) and enhances autophagy by binding to AMP-activated protein kinase (AMPK), thereby exerting antidepressant effects. Kaempferol 3-O-sophoroside holds promise for research in the fields of inflammation and neurodegenerative diseases.

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

Kaempferol 3-O-sophoroside Chemical Structure

Kaempferol 3-O-sophoroside Chemical Structure

CAS No. : 19895-95-5

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

Kaempferol 3-O-sophoroside is an orally active derivative of Kaempferol. It exhibits anti-inflammatory, analgesic, and antidepressant effects. Kaempferol 3-O-sophoroside is an inhibitor of the cell surface receptor toll-like receptor (TLR) 2/4 for High mobility group box 1 (HMGB1), and it also exerts anti-inflammatory effects by blocking the activation of NF-κB expression and the production of TNF-α. Kaempferol 3-O-sophoroside promotes the production of brain-derived neurotrophic factor (BDNF) and enhances autophagy by binding to AMP-activated protein kinase (AMPK), thereby exerting antidepressant effects. Kaempferol 3-O-sophoroside holds promise for research in the fields of inflammation and neurodegenerative diseases[1][2][3][4].

IC50 & Target

TLR2

 

TLR4

 

In Vitro

Kaempferol 3-O-sophoroside (5 μM, 48 h) does not affect the cell viability of human umbilical vein endothelial cells (HUVECs)[1].
Kaempferol 3-O-sophoroside (0-5 μM, 3 h) dose-dependently reduces barrier disruption in lipopolysaccharide (HY-D1056)-stimulated human umbilical vein endothelial cells (HUVECs), while it does not alter the integrity of the cell barrier when used alone[1].
Kaempferol 3-O-sophoroside (0-5 μM, 24 h) inhibits neutrophil adhesion to lipopolysaccharide (HY-D1056)-stimulated human umbilical vein endothelial cells (HUVECs) and suppresses neutrophil migration to HUVECs by blocking the activation of NF-κB and the production of TNF-α[1].

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

Cell Viability Assay[1]

Cell Line: Lipopolysaccharide (HY-D1056)-stimulated human umbilical vein endothelial cells (HUVECs)
Concentration: 0.005, 0.05, 0.5, 5 μM
Incubation Time: 48 h
Result: Did not effect cell via- bility At the concentration used (5 μM).

Cell Migration Assay [1]

Cell Line: Lipopolysaccharide (HY-D1056)-stimulated human umbilical vein endothelial cells (HUVECs)
Concentration: 0, 0.005, 0.05, 0.5, 5 μM
Incubation Time: 24 h
Result: Inhibited the binding of neutrophils to Lipopolysaccharides (HY-D1056)-stimulated endothelial cells and the transendothelial migration (TEM) of neutrophils.
In Vivo

Kaempferol 3-O-sophoroside (10 and 20 mg/kg, p.o., once daily for 20 days) binds to AMP-activated protein kinase (AMPK) to promote brain-derived neurotrophic factor (BDNF) production and autophagy enhancement in corticosterone (HY-B1618)-induced mouse depression model and chronic unpredictable mild stress (CUMS) model, ultimately achieving antidepressant effects[3].
Kaempferol 3-O-sophoroside (100 and 200 mg/kg, p.o., 30-minute administration duration) exhibits analgesic effects in the acetic acid-induced writhing mice model[4].

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

Animal Model: Acetic acid-induced writhing mice model[4]
Dosage: 50, 100, 200 mg/kg
Administration: Oral gavage (p.o.), administration duration of 30 minutes
Result: Caused dose-dependent inhibition of the writhing response induced by acetic acid.
Animal Model: Corticosterone (HY-B1618)-induced mouse depression model; Chronic unpredictable mild stress (CUMS) model[3]
Dosage: 10 and 20 mg/kg
Administration: Oral gavage (p.o.), once per day for 20 consecutive days
Result: Ameliorated weight loss, dyskinesia, and hippocampal volume reduction induced by Corticosterone and CUMS.
Molecular Weight

610.52

Formula

C27H30O16

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C1C(O[C@H]2[C@@H]([C@H]([C@@H]([C@@H](CO)O2)O)O)O[C@H]3[C@@H]([C@H]([C@@H]([C@@H](CO)O3)O)O)O)=C(C4=CC=C(O)C=C4)OC5=CC(O)=CC(O)=C15

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (163.79 mM; 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 1.6379 mL 8.1897 mL 16.3795 mL
5 mM 0.3276 mL 1.6379 mL 3.2759 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 and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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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 (4.09 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 (4.09 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:

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mg/kg

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(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 and 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: 99.84%

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 and 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 1.6379 mL 8.1897 mL 16.3795 mL 40.9487 mL
5 mM 0.3276 mL 1.6379 mL 3.2759 mL 8.1897 mL
10 mM 0.1638 mL 0.8190 mL 1.6379 mL 4.0949 mL
15 mM 0.1092 mL 0.5460 mL 1.0920 mL 2.7299 mL
20 mM 0.0819 mL 0.4095 mL 0.8190 mL 2.0474 mL
25 mM 0.0655 mL 0.3276 mL 0.6552 mL 1.6379 mL
30 mM 0.0546 mL 0.2730 mL 0.5460 mL 1.3650 mL
40 mM 0.0409 mL 0.2047 mL 0.4095 mL 1.0237 mL
50 mM 0.0328 mL 0.1638 mL 0.3276 mL 0.8190 mL
60 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6825 mL
80 mM 0.0205 mL 0.1024 mL 0.2047 mL 0.5119 mL
100 mM 0.0164 mL 0.0819 mL 0.1638 mL 0.4095 mL
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  • 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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Kaempferol 3-O-sophoroside
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