1. Apoptosis Anti-infection NF-κB
  2. Apoptosis Parasite NF-κB Bcl-2 Family Caspase
  3. Azadirachtin

Azadirachtin is an oral active triterpenoid compound with anticancer, antimalarial, anti-inflammatory, and insecticidal activities. Azadirachtin induces cell apoptosis through the mitochondrial pathway (by inhibiting Bcl-2/Bax ratio or activating Apaf-1 and caspase-3) or through death receptors (by inhibiting TNFR activation). Additionally, Azadirachtin exerts its anti-inflammatory effects by inhibiting NF-кB signaling pathway activation, and it exhibits insecticidal activity by inducing apoptosis in insect cells.

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Azadirachtin Chemical Structure

Azadirachtin Chemical Structure

CAS No. : 11141-17-6

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1 mg USD 72 In-stock
5 mg USD 275 In-stock
10 mg USD 420 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Azadirachtin:

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  • Biological Activity

  • Purity & Documentation

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Description

Azadirachtin is an oral active triterpenoid compound with anticancer, antimalarial, anti-inflammatory, and insecticidal activities. Azadirachtin induces cell apoptosis through the mitochondrial pathway (by inhibiting Bcl-2/Bax ratio or activating Apaf-1 and caspase-3) or through death receptors (by inhibiting TNFR activation). Additionally, Azadirachtin exerts its anti-inflammatory effects by inhibiting NF-кB signaling pathway activation, and it exhibits insecticidal activity by inducing apoptosis in insect cells[1][2][3][4][5][6].

IC50 & Target

Caspase 3

 

In Vitro

Azadirachtin (3-24 μM, 6 h) exerts its anti-inflammatory effects in Retinoic acid (HY-14649)-induced A549 (lung carcinoma) cells by inhibiting the NF-κB signaling pathway[3].
Azadirachtin (135 μM, 24 h) induces cell cycle arrest and mitochondria-mediated apoptosis in human cervical cancer (HeLa) cells[5].
Azadirachtin (50 μg/mL, 22-24 h) inhibits the early sporogonic development of Plasmodium berghei and blocks its transmission effect[6].

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

Western Blot Analysis[3]

Cell Line: Retinoic acid (HY-14649) -induced human lung carcinoma (A549) cells
Concentration: 0, 3, 6, 12, 24 μM
Incubation Time: 6 h
Result: Inhibited Retinoic acid (HY-14649)-induced NF-κB-dependent gene (ICAM1 (intercellular adhesion molecule 1) and cox2) expression
In Vivo

Azadirachtin (10 μg/kg, i.g., once daily, 3 days a week for 14 weeks) carcinogenesis in the DMBA (HY-W011845)-induced hamster buccal pouch (HBP) carcinoma model by modulating xenobiotic metabolism enzymes, DNA damage, antioxidants, invasion, and angiogenesis.[4].

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

Animal Model: DMBA (HY-W011845)-induced hamster buccal pouch (HBP) carcinoma model[4]
Dosage: 10 μg/kg
Administration: Intragastric administration (i.g.), once daily, 3 days a week for 14 weeks
Result: Significantly decreased the expression of CYP1A1, CYP1B1 and 8-OHdG and up-regulated RECK expression.
Significantly enhanced GSH and the activities of all the antioxidant enzymes.
Decreased phase I enzyme activities and elevated phase II enzyme activities in the pouch.
Molecular Weight

720.71

Formula

C35H44O16

CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

C[C@@]1([C@@]([C@@]2(O)C(OC)=O)([H])[C@]([C@H](C[C@H]3OC(C)=O)OC(/C(C)=C/C)=O)(CO2)[C@@]4([H])[C@](OC[C@@]43C(OC)=O)([H])[C@H]1O)[C@]([C@@H](O[C@]5([H])OC=C6)C[C@H]7[C@]56O)(O8)[C@]78C

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (138.75 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 1.3875 mL 6.9376 mL 13.8752 mL
5 mM 0.2775 mL 1.3875 mL 2.7750 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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Molecular Weight *

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: ≥ 2.5 mg/mL (3.47 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 (3.47 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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Animal weight
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g

Dosing volume
(per animal)

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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:
%
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 (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: 99.06%

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 1.3875 mL 6.9376 mL 13.8752 mL 34.6880 mL
5 mM 0.2775 mL 1.3875 mL 2.7750 mL 6.9376 mL
10 mM 0.1388 mL 0.6938 mL 1.3875 mL 3.4688 mL
15 mM 0.0925 mL 0.4625 mL 0.9250 mL 2.3125 mL
20 mM 0.0694 mL 0.3469 mL 0.6938 mL 1.7344 mL
25 mM 0.0555 mL 0.2775 mL 0.5550 mL 1.3875 mL
30 mM 0.0463 mL 0.2313 mL 0.4625 mL 1.1563 mL
40 mM 0.0347 mL 0.1734 mL 0.3469 mL 0.8672 mL
50 mM 0.0278 mL 0.1388 mL 0.2775 mL 0.6938 mL
60 mM 0.0231 mL 0.1156 mL 0.2313 mL 0.5781 mL
80 mM 0.0173 mL 0.0867 mL 0.1734 mL 0.4336 mL
100 mM 0.0139 mL 0.0694 mL 0.1388 mL 0.3469 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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Azadirachtin
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