1. Immunology/Inflammation NF-κB Apoptosis
  2. COX NF-κB Interleukin Related TNF Receptor
  3. Darutoside

Darutoside is an orally effective diterpene compound with significant anti-inflammatory, analgesic, wound healing promotion, and immunomodulatory activities. Darutoside reduces edema and pain responses by inhibiting the expression of COX-2 and the migration of inflammatory cells. It regulates macrophage polarization towards the M2 type by inhibiting the NF-κB pathway, alleviating inflammation and promoting wound healing. Through multi-target regulation of metabolic networks, Darutoside significantly alleviates acute gouty arthritis.

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Darutoside

Darutoside Chemical Structure

CAS No. : 59219-65-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
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100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Darutoside:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Darutoside

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Darutoside is an orally effective diterpene compound with significant anti-inflammatory, analgesic, wound healing promotion, and immunomodulatory activities. Darutoside reduces edema and pain responses by inhibiting the expression of COX-2 and the migration of inflammatory cells. It regulates macrophage polarization towards the M2 type by inhibiting the NF-κB pathway, alleviating inflammation and promoting wound healing. Through multi-target regulation of metabolic networks, Darutoside significantly alleviates acute gouty arthritis[1][2][3].

IC50 & Target[1][2][3]

COX-2

 

NF-κB

 

IL-1β

 

IL-8

 

IL-10

 

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
> 25 μM
Compound: 6
Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay
Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay
[PMID: 28302401]
RAW264.7 IC50
> 100 μM
Compound: 6
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 30 mins followed by LPS challenge measured after 24 hrs by Griess assay
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 30 mins followed by LPS challenge measured after 24 hrs by Griess assay
[PMID: 28302401]
In Vitro

Darutoside (0.1-1 mg/mL, 12 h) significantly inhibits the migration of RAW264.7 macrophages induced by LPS (HY-D1056)[1].
Darutoside (0.1-10 μM, 24 h) inhibits the M1-type macrophage polarization by suppressing the NF-κB signaling pathway (reducing the levels of p-IkK, p-IkB, and p-p65) [2].

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

In Vivo

Darutoside (0.2-2 mg/kg, local topical application, once a day for a total of 5 days) significantly reduces ear and paw edema in mice and decreases the number of convulsions induced by Acetic acid (HY-Y0319)1.
Darutoside (10-100 μM, local topical application, once daily for a total of 7 days) inhibits local inflammatory responses and significantly promotes wound healing in mouse skin[2].
Darutoside (40 mg/mL, p.o., 2 h before modeling, 6 h and 22 h after modeling for 3 doses) significantly alleviates acute gouty arthritis in rats by inhibiting inflammatory cell infiltration and release, promoting blood circulation and improving immunity[3].

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

Animal Model: Mouse ear swelling model, mouse paw swelling model and mouse writhing test established in young female Kunming mice with 8 weeks (18-22 g)[1]
Dosage: 0.2 and 2 mg/kg
Administration: Local topical application, once daily for 5 days
Result: Significantly reduced earlobe edema at 2 mg/kg.
Significantly alleviated paw edema induced by CFA (HY-153808), increased pain threshold, and reduced inflammatory cell infiltration.
Significantly reduce the number of convulsions induced by Acetic acid.
Animal Model: Full-thickness skin defect model established in 7-week-old male C57/BL6 mice[2]
Dosage: 10, 50, 100 μM (based on 2% Methylcellulose (HY-125861) gel)
Administration: Local topical application, once daily for 7 days
Result: Showed the most significant healing effect at 50 μM, with a significant increase in the wound healing rate.
Accelerated the migration and growth of epithelial cells at the wound edge.
Significantly reduced the expressions of Inosl, Il1b, Tnfa and Il6 in the wound tissue, and increased the expressions of M2 macrophage markers Mrc1, Tgfb and Il10.
Animal Model: Acute gouty arthritis model established in male Wistar rats (8 weeks old, weighing 150 g)[3]
Dosage: 40 mg/mL
Administration: Oral administration (p.o.), 2 h before modeling, 6 h and 22 h after modeling for 3 doses
Result: Significantly reduced the volume and thickness of the ankle joint.
Reduced the levels of serum IL-8, TNF-α, IL-1β, NF-κB and uric acid.
Significantly increased the level of the anti-inflammatory factor IL-10.
Molecular Weight

484.62

Formula

C26H44O8

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

C[C@]12[C@@]3([H])C(CC[C@]1([H])C(C)([C@H](O[C@]4([H])O[C@@H]([C@@H](O)[C@H](O)[C@H]4O)CO)CC2)C)=C[C@]([C@@H](O)CO)(C)CC3

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 (206.35 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 2.0635 mL 10.3174 mL 20.6347 mL
5 mM 0.4127 mL 2.0635 mL 4.1269 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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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 (5.16 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 (5.16 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).

*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: 99.89%

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 2.0635 mL 10.3174 mL 20.6347 mL 51.5868 mL
5 mM 0.4127 mL 2.0635 mL 4.1269 mL 10.3174 mL
10 mM 0.2063 mL 1.0317 mL 2.0635 mL 5.1587 mL
15 mM 0.1376 mL 0.6878 mL 1.3756 mL 3.4391 mL
20 mM 0.1032 mL 0.5159 mL 1.0317 mL 2.5793 mL
25 mM 0.0825 mL 0.4127 mL 0.8254 mL 2.0635 mL
30 mM 0.0688 mL 0.3439 mL 0.6878 mL 1.7196 mL
40 mM 0.0516 mL 0.2579 mL 0.5159 mL 1.2897 mL
50 mM 0.0413 mL 0.2063 mL 0.4127 mL 1.0317 mL
60 mM 0.0344 mL 0.1720 mL 0.3439 mL 0.8598 mL
80 mM 0.0258 mL 0.1290 mL 0.2579 mL 0.6448 mL
100 mM 0.0206 mL 0.1032 mL 0.2063 mL 0.5159 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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Darutoside
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HY-N6028
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