| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| Other Sizes |
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| ln Vitro |
Ivermectin is comprised of a mixture of two homologous molecules, ivermectin B1a (not less than 80%) and ivermectin B1b (not more than 20%), and is a member of the macrocyclic lactone class of avermectins. At a dose of 0.3 μg/ml, the primary component of ivermectin, ivermectin B1a, is inert, while at the same quantity, ivermectin B1b, the lesser component, causes 100% snail mortality[1].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Moderately well absorbed. Improved absorption with high fat meal. Ivermectin is metabolized in the liver, and ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1% of the administered dose excreted in the urine. The volume of distribution is 3 to 3.5 L/kg and it does not cross the blood-brain barrier. Metabolism / Metabolites Primarily hepatic. Ivermectin and/or its metabolites are excreted almost exclusively in the feces over an estimated 12 days, with less than 1 % of the administered dose excreted in the urine. Biological Half-Life Following oral administration, the half-life of ivermectin is approximately 18 hours. |
| Toxicity/Toxicokinetics |
Hepatotoxicity
Single dose therapy with ivermectin has been associated with a low rate of serum aminotransferase elevations. A single case of clinically apparent liver injury has been reported after ivermectin use (Case 1). The onset of injury occurred 1 month after a single dose and was characterized by a hepatocellular pattern of serum enzyme elevations without jaundice. Recovery was rapid and complete. In trials of ivermectin to prevent SARS-CoV-2 infection and to ameliorate the course of early as well as severe COVID-19, serum aminotransferase elevations were not uncommon but were no more frequent among patients receiving ivermectin than among those receiving placebo or a comparator drug. Likelihood score: D (possible rare cause of mild clinically apparent liver injury). Protein Binding 93% |
| References | |
| Additional Infomation |
Pharmacodynamics
Ivermectin is a semisynthetic, anthelminitic agent. It is an avermectin, a group of pentacyclic sixteen-membered lactones (i.e. a macrocyclic lactone disaccharide) derived from the soil bacterium _Streptomyces avermitilis_. Avermectins are potent and broad-spectrum anti-parasitic agents. |
| Molecular Formula |
C48H74O14
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|---|---|
| Molecular Weight |
875.09
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| Exact Mass |
874.508
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| CAS # |
71827-03-7
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| PubChem CID |
6321424
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| Appearance |
White to light yellow solid powder
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| LogP |
5.601
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
62
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| Complexity |
1680
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| Defined Atom Stereocenter Count |
20
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| 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
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| InChi Key |
AZSNMRSAGSSBNP-XPNPUAGNSA-N
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| 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+/m0/s1
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| Chemical Name |
(1R,4S,5'S,6R,6'R,8R,10E,12S,13S,14E,16E,20R,21R,24S)-6'-[(2S)-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
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (114.27 mM)
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|---|---|
| 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: ≥ 2.5 mg/mL (2.86 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1427 mL | 5.7137 mL | 11.4274 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.
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.
Insecticide Resistance Management in Burkina Faso and Côte D'Ivoire
CTID: NCT03074435
Phase: Phase 3 Status: Completed
Date: 2024-10-01
Products are for research use only; We do not sell to patients
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