Handelin
Based on 1 Customer Validation
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.
For research use only. We do not sell to patients.
- Purity: 99.55%
- CAS No.: 62687-22-3
- Formula: C32H40O8
- Molecular Weight:552.66
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CNE | IC50 |
>10 μM
Compound: 13
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Cytotoxicity against human CNE1 cells after 48 hrs by MTT assay
Cytotoxicity against human CNE1 cells after 48 hrs by MTT assay
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[PMID: 30726671] |
| CNE-2 | IC50 |
>10 μM
Compound: 13
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Cytotoxicity against human CNE2 cells after 48 hrs by MTT assay
Cytotoxicity against human CNE2 cells after 48 hrs by MTT assay
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[PMID: 30726671] |
| HONE1 cell line | IC50 |
>10 μM
Compound: 13
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Cytotoxicity against human HONE1 cells after 48 hrs by MTT assay
Cytotoxicity against human HONE1 cells after 48 hrs by MTT assay
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[PMID: 30726671] |
| HT-29 | IC50 |
>10 μM
Compound: 13
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Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
Cytotoxicity against human HT-29 cells after 48 hrs by MTT assay
|
[PMID: 30726671] |
| RAW264.7 | IC50 |
14.3 μM
Compound: 1
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Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS challenge measured after 20 hrs by EIA relative to control
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production administered 1 hr prior to LPS challenge measured after 20 hrs by EIA relative to control
|
[PMID: 24689881] |
| RAW264.7 | IC50 |
6.7 μM
Compound: 1
|
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production administered 30 mins prior to LPS challenge measured after 20 hrs by Griess assay
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production administered 30 mins prior to LPS challenge measured after 20 hrs by Griess assay
|
[PMID: 24689881] |
| SUNE1 | IC50 |
>10 μM
Compound: 13
|
Cytotoxicity against human SUNE1 cells after 48 hrs by MTT assay
Cytotoxicity against human SUNE1 cells after 48 hrs by MTT assay
|
[PMID: 30726671] |
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.
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Cell Line:RAW 264.7 cells
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Concentration:10 μM, 20 μM, 40 μM
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Incubation Time:5 hours
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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.
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Cell Line:RAW 264.7 cells
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Concentration:10 μM, 20 μM, 40 μM
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Incubation Time:
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley (SD) rats (150-170 g, 5 weeks old) injected with carrageenan[1]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:Oral administration; for 30 mintues
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Result:Inhibited acute inflammation in carrageenan-induced paw. The serum level of IL-1β was also inhibited.
Chemical Information
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CAS No. 62687-22-3
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Appearance Solid
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Molecular Weight 552.66
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Formula C32H40O8
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Color White to off-white
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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
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 8.33 mg/mL (15.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (1.50 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (1.50 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 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)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 | 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 |