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IVERMECTIN

Alias: MK-933; L-64047; MK 933; L64047; MK-0933; Noromectin; MK 933; Mectizan; MK 0933; Ivermectin; Ivomec; L 64047; Pandex.
Cat No.:V4365 Purity: ≥98%
Ivermectin (formerly known as MK-933; Noromectin;Mectizan;Ivomec; L-64047; Pandex) is aneffective and widely used antiparasitic medication approved for use in human and veterinary medicine against many types of parasites.
IVERMECTIN
IVERMECTIN Chemical Structure CAS No.: 70288-86-7
Product category: Parasite
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
Other Sizes
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ivermectin (formerly known as MK-933; Noromectin; Mectizan; Ivomec; L-64047; Pandex) is an effective and widely used antiparasitic medication approved for use in human and veterinary medicine against many types of parasites. It has been reported that Ivermectin may be used for COVID-19 treatment, but so far it has not approved by the FDA for the treatment of any viral infection. Ivermectin acts as a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin is used to treat head lice, scabies, river blindness, strongyloidiasis, and lymphatic filariasis, among others. Ivermectin and other avermectins (insecticides most frequently used in home-use ant baits) are macrocyclic lactones derived from the bacterium Streptomyces avermitilis. Ivermectin kills by interfering with nervous system and muscle function, in particular by enhancing inhibitory neurotransmission. Ivermectin is a mixture of mostly avermectin H2B1a with some avermectin H2B1b (CAS# 70209-81-3), which are macrolides from STREPTOMYCES avermitilis.

Biological Activity I Assay Protocols (From Reference)
Targets
HIV-1; HSV-1; BoHV-1; SARS-CoV-2;
ln Vitro
Ivermectin (MK-933) acts quickly and reversibly in the submicromolar range (EC50=250 nM), increasing the amplitude and delaying the deactivation of ATP-evoked P2X4 channel currents.Without altering the ion selectivity of P2X4 channels, ivermectin (MK-933) significantly boosts the potency of ATP and that of the typically low-potency agonist a,b-methylene-ATP in a use- and voltage-independent manner[1].
Ivermectin (MK-933) causes membrane hyperpolarization and muscular paralysis in the parasite by activating glutamate-gated chloride channels in its nerves and muscles[2].
The binding of Impα/β1 to NS5 is strongly inhibited by ivermectin (MK-933) (IC50=17 μM), but not the binding of Impβ1 by itself.Ivermectin (MK-933) exhibits strong antiviral activity against the dengue virus and HIV-1, which are both heavily dependent on importin α/β nuclear import with regard to the NS5 (non-structural protein 5) polymerase and HIV-1 integrase proteins, respectively[3].
References

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

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

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

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

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C48H74O14
Molecular Weight
875.1
CAS #
70288-86-7
Appearance
Typically exists as solids (or liquids in special cases) at room temperature
SMILES
CC[C@@H](C)[C@@H]1[C@H](CC[C@@]2(O1)C[C@@H]3C[C@H](O2)C/C=C(/[C@H]([C@H](/C=C/C=C/4\CO[C@H]5[C@@]4([C@@H](C=C([C@H]5O)C)C(=O)O3)O)C)O[C@H]6C[C@@H]([C@H]([C@@H](O6)C)O[C@H]7C[C@@H]([C@H]([C@@H](O7)C)O)OC)OC)\C)C
InChi Key
AZSNMRSAGSSBNP-ZGXOMDHGSA-N
InChi Code
InChI=1S/C48H74O14/c1-11-25(2)43-28(5)17-18-47(62-43)23-34-20-33(61-47)16-15-27(4)42(26(3)13-12-14-32-24-55-45-40(49)29(6)19-35(46(51)58-34)48(32,45)52)59-39-22-37(54-10)44(31(8)57-39)60-38-21-36(53-9)41(50)30(7)56-38/h12-15,19,25-26,28,30-31,33-45,49-50,52H,11,16-18,20-24H2,1-10H3/b13-12+,27-15+,32-14+/t25-,26+,28+,30+,31+,33-,34+,35+,36+,37+,38+,39+,40-,41+,42+,43-,44+,45-,47-,48-/m1/s1
Chemical Name
(1R,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,16E,20R,21R,24S)-6'-[(2R)-butan-2-yl]-21,24-dihydroxy-12-[(2R,4S,5S,6S)-5-[(2S,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
Synonyms
MK-933; L-64047; MK 933; L64047; MK-0933; Noromectin; MK 933; Mectizan; MK 0933; Ivermectin; Ivomec; L 64047; Pandex.
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : 100~250 mg/mL ( 114.27~285.68 mM )
Ethanol : ~100 mg/mL
H2O : < 0.1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.86 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (2.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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Solubility in Formulation 3: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (2.86 mM)


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.1427 mL 5.7136 mL 11.4273 mL
5 mM 0.2285 mL 1.1427 mL 2.2855 mL
10 mM 0.1143 mL 0.5714 mL 1.1427 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • IVM affects P2X4 deactivation kinetics but neither basal current nor membrane capacitance. [1].J Neurosci. 1999 Sep 1;19(17):7289-99.
  • IVM potentiates P2X4 but not P2X2 or P2X3 channel currents.A, Representative recordings of currents mediated by P2X4 channels expressed in oocytes. [1].J Neurosci. 1999 Sep 1;19(17):7289-99.
  • Properties of the IVM potentiation of P2X4 channel currents.[1].J Neurosci. 1999 Sep 1;19(17):7289-99.
  • Effect of α,β-methylene-ATP on homomeric P2X4 and heteromeric P2X4/P2X6 channels. [1].J Neurosci. 1999 Sep 1;19(17):7289-99.
  • IVM potentiates the high-selectivity (I1) but not the low-selectivity (I2) state of the P2X4 channel.A, Representative 3 μm ATP-evoked current from an oocyte expressing P2X4 channels; the solid bar indicates the period of ATP application. [1].J Neurosci. 1999 Sep 1;19(17):7289-99.
  • IVM potentiates P2X4 channel currents in a clonal mammalian cell line. [1].J Neurosci. 1999 Sep 1;19(17):7289-99.
  • Endogenous P2X channels in MNV and hippocampal CA1 neurons. [1].J Neurosci. 1999 Sep 1;19(17):7289-99.
  • P2X4 channels expressed in embryonic hippocampal neurons. [1].J Neurosci. 1999 Sep 1;19(17):7289-99.
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