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> Ivermectin [70288-86-7]

Ivermectin [70288-86-7]

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embalaje : 10mM/1mL

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Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.

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Ivermectin Estructura química

Ivermectin Estructura química

No. CAS : 70288-86-7

This product is a controlled substance and not for sale in your territory.

Based on 25 publication(s) in Google Scholar

Other Forms of Ivermectin:

  • Ivermectin (Standard) Obtener un presupuesto

Ver todos los productos específicos de isoformas Parasite:

Ver todas las isoformas
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

Ver todos los productos específicos de isoformas HIV:

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HIV HIV-1 HIV-2

Ver todos los productos específicos de isoformas HSV:

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HSV-1 HSV-2 HSV

Ver todos los productos específicos de isoformas Antibiotic:

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Aminoglycoside Glycopeptide Lipopeptide Macrolide Oxazolidinone Quinolone Tetracycline β-lactam
Descripciòn

Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import[1][2][3][4]. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19[5].

IC50 & Target[1]

HIV-1

 

HSV-1

 

BoHV-1

 

SARS-CoV-2

 

In Vitro

In the submicromolar range (EC50=250 nM) the action of Ivermectin (MK-933) is rapid and reversible, resulting in increased amplitude and slowed deactivation of P2X4 channel currents evoked by ATP[1].
Ivermectin (MK-933) markedly increases the potency of ATP and that of the normally low-potency agonist a,b-methylene-ATP in a use- and voltage-independent manner without changing the ion selectivity of P2X4 channels[1].
Ivermectin (MK-933) activates glutamate-gated chloride channels in the nerves and muscles of the parasite, leading to membrane hyperpolarization and muscle paralysis[2].
Ivermectin (MK-933) strongly inhibits the binding of Impα/β1 to NS5 (IC50=17 μM), but not of Impβ1 alone to NS5[3].
Ivermectin (MK-933) has potent antiviral activity towards both HIV-1 and dengue virus, both of which are strongly reliant on importin α/β nuclear import, with respect to the HIV-1 integrase and NS5 (non-structural protein 5) polymerase proteins respectively[3].

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

Ivermectin Related Antibodies
Ensayo clínico
Peso molecular

875.09

Fòrmula

C48H74O14
No. CAS

70288-86-7
Appearance

Solid

Color

White to off-white

SMILES

CO[C@H]1C[C@H](O[C@H]2[C@H](C)O[C@@H](O[C@H](/C(C)=C/C[C@@H]3C[C@H]4C[C@@]5(O[C@](15)(C(C)C)[C@@H](C)CC5)O3)[C@@H](C)/C=C/C=C6CO[C@@]7(15)[C@]\6(O)[C@H](C(O4)=O)C=C(C)[C@H]7O)C[C@@H]2OC)O[C@@H](C)[C@@H]1O.CO[C@H]8C[C@H](O[C@H]9[C@H](C)O[C@@H](O[C@H](/C(C)=C/C[C@@H]%10C[C@H]%11C[C@@]%12(O[C@](15)([C@@H](C)CC)[C@@H](C)CC%12)O%10)[C@@H](C)/C=C/C=C%13CO[C@@]%14(15)[C@]\%13(O)[C@H](C(O%11)=O)C=C(C)[C@H]%14O)C[C@@H]9OC)O[C@@H](C)[C@@H]8O
Structure Classification
  • Antibiotics
  • Disease Research
  • Antiviral
  • Antibiotics
  • Disease Research
  • Anti-parasitic
  • Antibiotics
  • Macrolide Antibiotics
Initial Source
  • Microorganisms

Streptomyces avermitilis
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 250 mg/mL (285.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.1427 mL 5.7137 mL 11.4274 mL
5 mM 0.2285 mL 1.1427 mL 2.2855 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.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (2.86 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% Corn Oil

    Solubility: ≥ 2.08 mg/mL (2.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 3.33 mg/mL (3.81 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

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).
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.
Pureza y Documentación

Purity: 98.01%

SDS (623 KB)

COA (266 KB) HNMR (412 KB) RP-HPLC (215 KB)

Instrucciones de manejo (2659 KB)
Referencias

  • [1]. Khakh BS, et al. Allosteric control of gating and kinetics at P2X(4) receptor channels. J Neurosci. 1999 Sep 1;19(17):7289-99.  [Content Brief]

    [2]. Priel A, et al. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004 Mar;123(3):281-93.  [Content Brief]

    [3]. Wagstaff KM, et al. Ivermectin is a specific inhibitor of importin α/β-mediated nuclear import able to inhibit replication of HIV-1 and dengue virus. Biochem J. 2012 May 1;443(3):851-6.  [Content Brief]

    [4]. Raza S, et al. Ivermectin Inhibits Bovine Herpesvirus 1 DNA Polymerase Nuclear Import and Interferes with Viral Replication. Microorganisms. 2020 Mar 13;8(3). pii: E409.  [Content Brief]

    [5]. Khan Sharun, et al. Ivermectin, a New Candidate Therapeutic Against SARS-CoV-2/COVID-19. Ann Clin Microbiol Antimicrob. 2020 May 30;19(1):23.  [Content Brief]

  • [1]. Khakh BS, et al. Allosteric control of gating and kinetics at P2X(4) receptor channels. J Neurosci. 1999 Sep 1;19(17):7289-99.

    [2]. Priel A, et al. Mechanism of ivermectin facilitation of human P2X4 receptor channels. J Gen Physiol. 2004 Mar;123(3):281-93.

    [3]. Wagstaff KM, et al. Ivermectin is a specific inhibitor of importin α/β-mediated nuclear import able to inhibit replication of HIV-1 and dengue virus. Biochem J. 2012 May 1;443(3):851-6.

    [4]. Raza S, et al. Ivermectin Inhibits Bovine Herpesvirus 1 DNA Polymerase Nuclear Import and Interferes with Viral Replication. Microorganisms. 2020 Mar 13;8(3). pii: E409.

    [5]. Khan Sharun, et al. Ivermectin, a New Candidate Therapeutic Against SARS-CoV-2/COVID-19. Ann Clin Microbiol Antimicrob. 2020 May 30;19(1):23.

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 1.1427 mL 5.7137 mL 11.4274 mL 28.5685 mL
5 mM 0.2285 mL 1.1427 mL 2.2855 mL 5.7137 mL
10 mM 0.1143 mL 0.5714 mL 1.1427 mL 2.8568 mL
15 mM 0.0762 mL 0.3809 mL 0.7618 mL 1.9046 mL
20 mM 0.0571 mL 0.2857 mL 0.5714 mL 1.4284 mL
25 mM 0.0457 mL 0.2285 mL 0.4571 mL 1.1427 mL
30 mM 0.0381 mL 0.1905 mL 0.3809 mL 0.9523 mL
40 mM 0.0286 mL 0.1428 mL 0.2857 mL 0.7142 mL
50 mM 0.0229 mL 0.1143 mL 0.2285 mL 0.5714 mL
60 mM 0.0190 mL 0.0952 mL 0.1905 mL 0.4761 mL
80 mM 0.0143 mL 0.0714 mL 0.1428 mL 0.3571 mL
100 mM 0.0114 mL 0.0571 mL 0.1143 mL 0.2857 mL
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Ivermectin Related Classifications

  • Infection Cancer
  • Cancer Targeted Therapy Cancer Immunotherapy Cancer Metabolism and Metastasis
  • Anti-infection Autophagy
  • Dengue virus Flavivirus Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Bacterial
Help & FAQs

Keywords:

Ivermectin70288-86-7MK-933 CD-5024 K-237MK933MK 933CD5024CD 5024CD-5024K237K 237K-237Dengue virusFlavivirusParasiteHIVMitophagyHSVSARS-CoVAntibioticAutophagyBacterialDENVHuman immunodeficiency virusMitochondrial AutophagyHerpes simplex virusSARS coronavirusInhibitorinhibitorinhibit

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