| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Chloride channels in invertebrate nerve and muscle cells. The parent compound, Ivermectin, is known to bind to and activate glutamate-gated chloride channels (GluCls) in nematodes and arthropods, leading to hyperpolarization of the cell membrane, flaccid paralysis, and death of the parasite. It may also interact with other ligand-gated chloride channels, such as those gated by GABA. As a structural analogue, 7-O-Methyl Ivermectin B1a may retain some ability to interact with these channels, though research is ongoing.
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| ln Vitro |
Detailed in vitro activity data for 7-O-Methyl Ivermectin B1a is not extensively available in the search results. Ivermectin B1a, the parent compound, is a potent anthelmintic agent. It exhibits strong activity against a wide range of parasites, including nematodes (roundworms) and arthropods (insects, mites). It is effective against parasites such as Onchocerca volvulus, Strongyloides stercoralis, and Sarcoptes scabiei. The mechanism involves potentiating chloride ion influx, leading to paralysis and death of the parasite. 7-O-Methyl Ivermectin B1a has been shown to have little or no activity against bacteria, fungi, or parasites.
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| ln Vivo |
In vivo activity data for 7-O-Methyl Ivermectin B1a is not detailed. The parent compound, Ivermectin, is highly effective in vivo against a wide variety of parasites in both veterinary and human medicine. In animal models, Ivermectin effectively clears nematode and arthropod infections at low dose rates (300 ug/kg or less). In humans, Ivermectin is the standard treatment for onchocerciasis (river blindness) and strongyloidiasis. The 7-O-Methyl derivative is a structural analog and may not demonstrate the same level of in vivo efficacy.
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| Enzyme Assay |
Ivermectin-based compounds are sometimes studied using non-cell systems to measure their ability to interact with target ion channels. One approach is to use membrane potential-sensitive fluorescent dyes to detect changes in chloride flux in cell-free assays using isolated membrane vesicles containing expressed glutamate-gated chloride channels. For binding studies, the compound can be tested for its ability to displace radiolabeled ivermectin from parasite membrane preparations. However, 7-O-Methyl Ivermectin B1a is primarily used as a research reagent.
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| Cell Assay |
Ivermectin B1a is known to inhibit proliferation of several cancer cell lines, including breast, ovarian, and leukemia cells. Its cytotoxic effects in vitro are typically assessed using standard cell viability assays. However, the 7-O-Methyl derivative has shown little or no activity against bacteria, fungi, or parasites.
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| Animal Protocol |
Ivermectin B1a has been studied for antiparasitic efficacy in animal models of parasitic infection. It is typically administered orally or subcutaneously. The 7-O-Methyl derivative is not commonly used for in vivo efficacy studies. It is instead used as a reference standard or impurity marker for quality control of Ivermectin production.
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| ADME/Pharmacokinetics |
Ivermectin B1a has a half-life of approximately 16-18 hours in humans. The compound is highly lipophilic and extensively distributed throughout the body, with high concentrations found in the liver, fat, and tissues. It is metabolized in the liver, primarily by CYP3A4, and is excreted primarily in the feces. For 7-O-Methyl Ivermectin B1a, it is soluble in DMSO, and long-term storage should be at -20degC.
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| Toxicity/Toxicokinetics |
The toxicity of Ivermectin itself is low at therapeutic doses. The most common adverse effects in humans are related to the immune response to dying parasites rather than direct drug toxicity. At very high doses (e.g., accidental overdoses), ivermectin can cause neurotoxicity, as it can cross the blood-brain barrier and interfere with GABAergic neurotransmission. This results in symptoms like ataxia, tremors, and seizures. As an impurity, 7-O-Methyl Ivermectin B1a is not intended for therapeutic use and is generally considered non-toxic at the levels it is present in drug substance.
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| Additional Infomation |
Ivermectin is the active ingredient in several FDA-approved drugs for parasitic infections, including Stromectol (oral) and Sklice (topical). It is on the WHO Model List of Essential Medicines. Ivermectin has also gained attention as a potential antiviral and anticancer agent, though these uses are not FDA-approved. The discovery of Ivermectin led to the Nobel Prize in Physiology or Medicine in 2015. 7-O-Methyl Ivermectin B1a is a research compound used as an impurity reference standard.
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| Molecular Formula |
C49H76O14
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|---|---|
| Molecular Weight |
889.12
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| Appearance |
White to off-white solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1247 mL | 5.6235 mL | 11.2471 mL | |
| 5 mM | 0.2249 mL | 1.1247 mL | 2.2494 mL | |
| 10 mM | 0.1125 mL | 0.5624 mL | 1.1247 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.
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