2. NF-κB PI3K/Akt/mTOR TGF-beta/Smad Stem Cell/Wnt
  3. NF-κB PI3K Akt TGF-beta/Smad
  4. Micheliolide

Micheliolide is a sesquiterpene lactone with anti-cancer and anti-inflammatory effects, which is derived from Michelia compressa and Michelia champaca. Micheliolide can attenuate high glucose-stimulated NF-κB activation, IκBα degradation, and the expression of MCP-1, TGF-β1, and FN in mouse mesangial cells. Micheliolide inhibits LPS (HY-D1056)-induced activation of NF-κB and PI3K/Akt/p70S6K pathways to play an anti-inflammatory role. Micheliolide inhibits dextran sodium sulphate (DSS) (HY-116282)-induced inflammatory intestinal disease, colitis-associated cancer and rheumatic arthritis.

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Micheliolide 構造式

Micheliolide 構造式

CAS 番号 : 68370-47-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 在庫あり
Solution
10 mM * 1 mL in DMSO USD 165 在庫あり
Solid
1 mg USD 50 在庫あり
5 mg USD 150 在庫あり
10 mg USD 240 在庫あり
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Based on 4 publication(s) in Google Scholar

Other Forms of Micheliolide:

Micheliolide 関連抗体

Top Publications Citing Use of Products

NF-κB アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

PI3K アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Akt アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Akt Akt1 Akt2 Akt3

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製品説明

Micheliolide is a sesquiterpene lactone with anti-cancer and anti-inflammatory effects, which is derived from Michelia compressa and Michelia champaca. Micheliolide can attenuate high glucose-stimulated NF-κB activation, IκBα degradation, and the expression of MCP-1, TGF-β1, and FN in mouse mesangial cells. Micheliolide inhibits LPS (HY-D1056)-induced activation of NF-κB and PI3K/Akt/p70S6K pathways to play an anti-inflammatory role. Micheliolide inhibits dextran sodium sulphate (DSS) (HY-116282)-induced inflammatory intestinal disease, colitis-associated cancer and rheumatic arthritis[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
HL-60 IC50
5.5 μM
Compound: 9, MCL
Cytotoxicity against human HL60 cells after 18 hrs by annexin-V labeling-based flow cytometry
Cytotoxicity against human HL60 cells after 18 hrs by annexin-V labeling-based flow cytometry
[PMID: 22985027]
体外実験

Micheliolide (0.2-10 μM, 24 h) decreases the proliferation of mesangial cells and the production of MCP-1, TGF-β1, FN increased by a high concentration of glucose (HG) and suppresses the HG-induced degradation of IκBα[1].
Micheliolide (1-10 μM, 18 h) does not affect the growth and apoptosis of Raw264.7. I[2].
Micheliolide (1-10 μM, 3-18 h) inhibits LPS-triggered inflammatory responses in mouse macrophages, dendritic cells (DCs), human monocytic cell line THP-1, human CD14+ monocytes and inhibits LPS-induced NF-κB and PI3K/Akt/p70S6K activation[2][3].

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

Micheliolide 関連抗体

Real Time qPCR[2]

Cell Line: Mouse macrophages and dendritic cells
Concentration: 1-10 μM
Incubation Time: 3-18 h
Result: Inhibited LPS-induced IL-6, TNF-α, IL-1β, MCP-1, IFN-β and IL-10 production in Raw264.7 and mouse primary peritoneal macrophages.

Western Blot Analysis[2]

Cell Line: Raw264.7 cells
Concentration: 10 μM
Incubation Time: 0-180 min
Result: Inhibited LPS-induced phosphorylation of IκBα (Ser32/36) in Raw264.7.
体内実験

Micheliolide (10 or 20 mg/kg, i.p., a single dose for 2 h) attenuates the secretion of serum cytokines and protects against lung and liver tissue damage in LPS (10mg/kg, i.p., a single dose for 2 h)-challenged mice[2].
Micheliolide (10 or 20 mg/kg, i.p., a single dose for 6 days) enhances the survival rate in mice following lethal septic shock[2].
Micheliolide (30 mg/kg, i.p., every two days for 63 days) reduces swelling of the paws and suppresses the degeneration of articular cartilage in collagen-induced arthritis mice[4].

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

Animal Model: Acute peritonitis mouse model[2]
Dosage: 10 or 20 mg/kg
Administration: i.p., a single dose for 2 h
Result: Suppressed LPS-induced production of proinflammatory cytokines, chemokines and IFN in macrophages and DCs, showing clearer alveolar wall and less inflammatory cell infiltration.
Animal Model: Septic shock mouse model[2]
Dosage: 10 or 20 mg/kg
Administration: i.p., a single dose for 6 days
Result: Protected mice against septic shock following lethal LPS challenge.
Animal Model: Collagen-induced arthritis mice[4]
Dosage: 30 mg/kg
Administration: i.p., every two days for 63 days
Result: Remited the pathological changes of collagen-induced arthritis and recovered the expression levels of M-CSF, TIMP-1 and C5/C5a in collagen-induced arthritis mice.
分子量

248.32

分子式

C15H20O3
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C(O[C@@]1([H])[C@@]2([H])CCC(C)=C3CC[C@@](C)(O)[C@@]31[H])C2=C
Structure Classification
Initial Source
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 50 mg/mL (201.35 mM; ultrasonic and warming and heat to 60°C; 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 4.0271 mL 20.1353 mL 40.2706 mL
5 mM 0.8054 mL 4.0271 mL 8.0541 mL
10 mM 0.4027 mL 2.0135 mL 4.0271 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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一般には略語で表示されます：C1V1 = C2V2

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体内:

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 (10.07 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 (10.07 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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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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).
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.
純度とドキュメンテーション

純度: 99.84%

COA (260 KB) HNMR (260 KB) LCMS (262 KB)

取扱説明書 (2659 KB)
参考文献

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 4.0271 mL 20.1353 mL 40.2706 mL 100.6765 mL
5 mM 0.8054 mL 4.0271 mL 8.0541 mL 20.1353 mL
10 mM 0.4027 mL 2.0135 mL 4.0271 mL 10.0677 mL
15 mM 0.2685 mL 1.3424 mL 2.6847 mL 6.7118 mL
20 mM 0.2014 mL 1.0068 mL 2.0135 mL 5.0338 mL
25 mM 0.1611 mL 0.8054 mL 1.6108 mL 4.0271 mL
30 mM 0.1342 mL 0.6712 mL 1.3424 mL 3.3559 mL
40 mM 0.1007 mL 0.5034 mL 1.0068 mL 2.5169 mL
50 mM 0.0805 mL 0.4027 mL 0.8054 mL 2.0135 mL
60 mM 0.0671 mL 0.3356 mL 0.6712 mL 1.6779 mL
80 mM 0.0503 mL 0.2517 mL 0.5034 mL 1.2585 mL
100 mM 0.0403 mL 0.2014 mL 0.4027 mL 1.0068 mL
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Micheliolide Related Classifications

  • Molarity Calculator

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The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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:

Micheliolide68370-47-8NF-κBPI3KAktTGF-beta/SmadNuclear factor-κBNuclear factor-kappaBPhosphoinositide 3-kinasePKBProtein kinase BTransforming growth factor betasesquiterpene lactoneanti-canceranti-inflammatoryIκBαMCP-1TGF-β1FNmouse mesangial cellsinflammatory intestinal diseasecolitis-associated cancerrheumatic arthritisInhibitorinhibitorinhibit

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