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  3. Emamectin Benzoate

Emamectin Benzoate  (Synonyms: MK-244)

Cat. No.: HY-B0837 Purity: 99.71%
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Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. Emamectin Benzoate is one of semi-synthetic derivative of Avermectin (HY-15311) with a broadspectrum of insecticidal and acaricidal activity. Emamectin Benzoate induces ROS-mediated DNA damage and cell apoptosis. Emamectin Benzoate, a mixture of the natural Emamectin B1a benzoate and Emamectin B1b benzoate, has the main component of Emamectin B1a benzoate.

For research use only. We do not sell to patients.

Emamectin Benzoate Chemical Structure

Emamectin Benzoate Chemical Structure

CAS No. : 155569-91-8

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10 mM * 1 mL in DMSO USD 44 In-stock
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500 mg USD 80 In-stock
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Description

Emamectin Benzoate (MK-244) is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. Emamectin Benzoate is one of semi-synthetic derivative of Avermectin (HY-15311) with a broadspectrum of insecticidal and acaricidal activity. Emamectin Benzoate induces ROS-mediated DNA damage and cell apoptosis. Emamectin Benzoate, a mixture of the natural Emamectin B1a benzoate and Emamectin B1b benzoate, has the main component of Emamectin B1a benzoate[1][2].

IC50 & Target

Mite

 

In Vitro

Emamectin Benzoate (MK-244; 2.5-40 μM; 12 and 24 h) decreases cell viability in a time- and dose-dependent manner[1].
? Emamectin Benzoate (2.5-20 μM; 24 hours) induces apoptosis and DNA damage in 16HBE cells. Emamectin Benzoate induces ROS generation in 16HBE cells[1].
? Emamectin Benzoate (2.5-20 μM; 12 hours) increases the amounts of cytochrome-c, caspase-3, cas-pase-9, cleaved-PARP, Bax/Bcl-2[1].
? Emamectin Benzoate (2.5, 5, 10, 15 μM; 72 h) inhibits cell viability with an IC50 of 3.72 μM in Trichoplusia Tn5B1-4 cell. Emamectin Benzoat induces chromatin condensation in nuclei and cell apoptosis[2].

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

Cell Viability Assay[1]

Cell Line: human normal bronchial epithelial cell line 16HBE
Concentration: 2.5, 5, 7.5,10,15, 20, 40 μM
Incubation Time: 12 and 24 hours
Result: Decreased cell viability in a time- and dose-dependent manner wirh IC50s of 11.88 μM and 9.67 μM in 12 and 24 hours, respectively.

Apoptosis Analysis[1]

Cell Line: human normal bronchial epithelial cell line 16HBE
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 24 hours
Result: Induced apoptosis and caused chromatin shrinkage and nuclear fragmentation.

Western Blot Analysis[1]

Cell Line: human normal bronchial epithelial cell line 16HBE
Concentration: 2.5, 5, 10, 20 μM
Incubation Time: 12 hours
Result: Increased the amounts of cytochrome-c, caspase-3, cas-pase-9, cleaved-PARP, Bax/Bcl-2.
In Vivo

Emamectin Benzoate (MK-244; oral; 25-100 mg/kg/day; for 14 days) causes a marked induction of oxidative damage in liver tissue[3].

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

Animal Model: 10 weeks old Swiss albino male mice (25-30 g)[3]
Dosage: 25, 50, 100 mg/kg
Administration: Oral; daily; for 14 days
Result: Caused a marked induction of oxidative damage in liver tissue as demonstrated by an increased level of TBARS and reduced GSH level.
Molecular Weight

1008.24(Based on Emamectin B1a Benzoate)

Formula

C49H75NO13.C7H6O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C[C@H]1O[C@@H](O[C@@]2([H])[C@H](C)O[C@@H](O[C@]([C@@H](C)/C=C/C=C3CO[C@@]4([H])[C@]\3(O)[C@H]5C=C(C)[C@H]4O)([H])/C(C)=C/C[C@@H]6C[C@H](OC5=O)C[C@]7(C=C[C@H](C)[C@@H](C(C)C)O7)O6)C[C@@H]2OC)C[C@@H](OC)[C@@H]1NC.C[C@H]8O[C@@H](O[C@@]9([H])[C@H](C)O[C@@H](O[C@]([C@@H](C)/C=C/C=C%10CO[C@@]%11([H])[C@]\%10(O)[C@H]%12C=C(C)[C@H]%11O)([H])/C(C)=C/C[C@@H]%13C[C@H](OC%12=O)C[C@]%14(C=C[C@H](C)[C@@H]([C@H](CC)C)O%14)O%13)C[C@@H]9OC)C[C@@H](OC)[C@@H]8NC.O=C(O)C%15=CC=CC=C%15

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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  • 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: ≥ 2.08 mg/mL (Infinity mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (Infinity mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Purity & Documentation

Purity: 99.71%

References
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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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Emamectin Benzoate
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