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Handelin is a guaianolide dimer from Chrysanthemum boreale that has potent anti-inflammatory activity by down-regulating NF-κB signaling and pro-inflammatory cytokine production.

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Handelin Chemical Structure

Handelin Chemical Structure

CAS No. : 62687-22-3

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1 mg USD 80 In-stock
5 mg USD 220 In-stock
10 mg USD 360 In-stock
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Description

Handelin is a guaianolide dimer from Chrysanthemum boreale that has potent anti-inflammatory activity by down-regulating NF-κB signaling and pro-inflammatory cytokine production[1].

In Vitro

Handelin (Compound 1; 10-40 μM; RAW 264.7 cells) treatment suppresses the LPS-induced (1 μg/mL) overexpression of iNOS and COX-2 protein levels in a concentration-dependent manner. Handelin also suppresseS the induction of pro-inflammatory cytokines TNF-α and IL-1β in LPS-stimulated RAW 264.7 cells. Handelin also suppresses the activation of mitogen-activated protein kinases, including ERK and JNK signaling[1].
Handelin (Compound 1; 10-40 μM; RAW 264.7 cells) treatment significantly reduces the iNOS and COX-2 mRNA levels in LPS- stimulated RAW 264.7 cells. The transcriptional activity of NF-κB stimulated with LPS is also suppressed by Handelin. In addition, the LPS-stimulated upregulation of miRNA-155 expression is suppressed by Handelin[1].

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

RT-PCR[1]

Cell Line: RAW 264.7 cells
Concentration: 10 μM, 20 μM, 40 μM
Incubation Time: 5 hours
Result: iNOS and COX-2 mRNA levels were significantly reduced. The transcriptional activity of NF-κB stimulated with LPS was also suppressed and the LPS-stimulated upregulation of miRNA-155 expression was also suppressed.

Western Blot Analysis[1]

Cell Line: RAW 264.7 cells
Concentration: 10 μM, 20 μM, 40 μM
Incubation Time:
Result: Suppressed the LPS-induced overexpression of iNOS and COX-2 protein levels in a concentration-dependent manner. Suppressed the induction of pro-inflammatory cytokines TNF-α and IL-1β, and also also suppressed the activation of mitogen-activated protein kinases, including ERK and JNK signaling in LPS-stimulated RAW 264.7 cells.
In Vivo

Handelin (Compound 1; 10-20 mg/kg; oral administration; for 30 mintues; male Sprague-Dawley rats) treatment inhibits acute inflammation in carrageenan-induced paw edema model. The serum level of IL-1β is also inhibited by Handelin in a carrageenan-induced paw edema model [1].

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

Animal Model: Male Sprague-Dawley (SD) rats (150-170 g, 5 weeks old) injected with carrageenan[1]
Dosage: 10 mg/kg, 20 mg/kg
Administration: Oral administration; for 30 mintues
Result: Inhibited acute inflammation in carrageenan-induced paw. The serum level of IL-1β was also inhibited.
Molecular Weight

552.66

Formula

C32H40O8

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@]([C@]([C@@](OC1=O)([H])[C@@](C1=C)([H])CC[C@]2(O)C)([H])[C@@]32C4)(C=C3)[C@]54[C@@]([C@H]6OC(C)=O)([H])[C@]([C@](C(C)=CC7)([H])[C@]7([H])[C@](C)(O)C6)([H])OC5=O

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 : 16.67 mg/mL (30.16 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 1.8094 mL 9.0472 mL 18.0943 mL
5 mM 0.3619 mL 1.8094 mL 3.6189 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: 1.67 mg/mL (3.02 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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: 1.67 mg/mL (3.02 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 1.67 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 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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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
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%
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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: 99.44%

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 1.8094 mL 9.0472 mL 18.0943 mL 45.2358 mL
5 mM 0.3619 mL 1.8094 mL 3.6189 mL 9.0472 mL
10 mM 0.1809 mL 0.9047 mL 1.8094 mL 4.5236 mL
15 mM 0.1206 mL 0.6031 mL 1.2063 mL 3.0157 mL
20 mM 0.0905 mL 0.4524 mL 0.9047 mL 2.2618 mL
25 mM 0.0724 mL 0.3619 mL 0.7238 mL 1.8094 mL
30 mM 0.0603 mL 0.3016 mL 0.6031 mL 1.5079 mL
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Handelin 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.

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Handelin
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