| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| Targets |
Milbemycin oxime targets glutamate-gated chloride channels in parasites. By selectively binding to these channels, the compound causes increased chloride influx into parasite nerve and muscle cells, leading to hyperpolarization, paralysis, and death of the parasite. Milbemycin oxime consists of milbemycin A4 and A3, both of which contribute to its antiparasitic activity. The compound is active against a wide range of parasites, including intestinal nematodes, pulmonary and cardiac helminths. Its broad-spectrum activity makes it effective against worms (anthelmintic) and mites (miticide). The compound's selectivity for parasite glutamate-gated chloride channels over mammalian ion channels contributes to its safety profile. Milbemycin oxime is an orally active macrolide that serves as a potent inhibitor of parasite activity.
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| ln Vitro |
In vitro, milbemycin oxime demonstrates potent antiparasitic activity. The compound selectively binds to glutamate-gated chloride channels, leading to paralysis and death of various parasites. In vitro assays using parasite cultures or isolated parasite tissues can assess the compound's efficacy against specific parasites. The compound's activity against intestinal nematodes, pulmonary and cardiac helminths has been demonstrated in vitro. Milbemycin oxime's broad-spectrum activity makes it effective against a wide range of parasites. The compound's mechanism of action involves increased chloride influx into parasite cells, leading to hyperpolarization and paralysis. The compound's potency against various parasites supports its use as a veterinary antiparasitic agent.
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| ln Vivo |
In vivo, milbemycin oxime demonstrates efficacy in treating and preventing parasitic infections in animals. It is commonly used to prevent heartworms and control disease caused by roundworms, hookworms in dogs and cats and certain whipworms in dogs. The compound is administered orally and is effective against a wide range of parasites. Milbemycin oxime has been shown to be effective in experimentally induced infections in dogs. The compound's broad-spectrum activity and oral bioavailability make it a valuable veterinary antiparasitic agent. Milbemycin oxime is used as a veterinary drug from the group of milbemycins. The compound is practically odorless, appearing as a white to pale yellow powder, with a melting point of 169.6-177.4°C.
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| Enzyme Assay |
In vitro assays for milbemycin oxime typically employ parasite cultures or isolated parasite tissues to assess antiparasitic activity. Parasites such as nematodes or mites are cultured in appropriate media and treated with milbemycin oxime at various concentrations. Parasite viability is assessed by observing motility, morphology, or by using vital dyes. The EC₅₀ or LC₅₀ is calculated from dose-response curves. For studies investigating the mechanism of action, electrophysiological techniques such as patch-clamp are used to measure chloride currents through glutamate-gated chloride channels in parasite cells. For studies investigating the compound's binding to glutamate-gated chloride channels, radioligand binding assays may be used with membrane preparations from parasites.
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| Cell Assay |
Cellular assays for milbemycin oxime typically employ parasite cell lines or primary parasite cells to evaluate antiparasitic activity. Parasite cells are cultured in appropriate media and treated with milbemycin oxime at various concentrations. Cell viability is assessed using standard assays such as MTT or by observing motility. For studies investigating the mechanism of action, changes in membrane potential or chloride flux are measured using fluorescent indicators or electrophysiological techniques. The compound's effects on mammalian cells can also be assessed to evaluate selectivity and potential toxicity. Cell viability and proliferation are assessed using standard cytotoxicity assays.
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| Animal Protocol |
In vivo animal experiments for milbemycin oxime employ various animal models of parasitic infection. For heartworm prevention studies, dogs are infected with heartworm larvae and treated with milbemycin oxime, and the prevention of heartworm infection is assessed. For roundworm and hookworm control studies, dogs or cats are infected with these parasites and treated with milbemycin oxime, and fecal egg counts are measured. For whipworm control studies, dogs are infected with whipworms and treated with milbemycin oxime. Pharmacokinetic studies are also conducted in animals to assess absorption, distribution, metabolism, and excretion. Dosing regimens vary depending on the parasite and animal species.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of milbemycin oxime have been characterized in dogs and other animals. After oral administration of milbemycin oxime in dogs, peak plasma levels occur at about 2-4 hours, and decline with a half-life of the unmetabolised milbemycin oxime of 1-4 days. Bioavailability is about 80%. Oral administration of milbemycin oxime tablets resulted in a peak concentration (Cmax) of 0.33 ± 0.07 µg/mL at 2.47 ± 1.90 h, with a mean residence time (MRT) of 21.96 hours. Milbemycin oxime nanoemulsion has a favorable pharmacokinetic profile, including rapid absorption, wide distribution, and slow elimination in Pekingese dogs. The compound's pharmacokinetics support its use as an orally administered veterinary antiparasitic agent.
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| Toxicity/Toxicokinetics |
The toxicity profile of milbemycin oxime is favorable for veterinary use. The compound is generally well-tolerated in dogs and cats at therapeutic doses. The oral LD₅₀ in mice is 1000-1500 mg/kg. Common adverse effects are rare but may include vomiting, diarrhea, or lethargy in some animals. The compound should be used with caution in animals with known hypersensitivity to milbemycins. The compound's safety in pregnant or lactating animals has been studied, and it is generally considered safe for use when indicated. Milbemycin oxime is a veterinary drug and is not approved for use in humans. The compound's selectivity for parasite glutamate-gated chloride channels over mammalian ion channels contributes to its safety profile.
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| Additional Infomation |
Milbemycin oxime is a broad-spectrum antiparasitic drug used in veterinary medicine. It consists of milbemycin A4 and A3 and selectively binds to glutamate-gated chloride channels, leading to paralysis and death of parasites. Milbemycin oxime is active against worms (anthelmintic) and mites (miticide). It is commonly used to prevent heartworms and control disease caused by roundworms, hookworms in dogs and cats and certain whipworms in dogs. After oral administration in dogs, peak plasma levels occur at about 2-4 hours, with a half-life of 1-4 days and bioavailability of about 80%. Milbemycin oxime has a molecular weight of 1097.38. It is a veterinary drug from the group of milbemycins.
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| Molecular Formula |
C32H45NO7.C31H43NO7
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| Molecular Weight |
1097.37782
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| CAS # |
129496-10-2
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| Related CAS # |
51570-36-6;129496-10-2 (oxime);114177-14-9 (A3 Oxime);
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| Appearance |
White to off-white solid powder
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| Melting Point |
169.6-177.4°
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| Flash Point |
412℃
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| LogP |
20.794
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| SMILES |
[C@@]12(C=C(C)/C(=N\O)/[C@@]3([H])OCC(=CC=C[C@H](C)CC(C)=CC[C@]4([H])C[C@@]([H])(C[C@]5(CC[C@H](C)[C@@H](CC)O5)O4)OC1=O)[C@@]23O)[H].[C@@]12(C=C(C)/C(=N/O)/[C@]3(OCC(=CC=C[C@H](C)CC(=CC[C@]4([H])C[C@@]([H])(C[C@]5(CC[C@H](C)[C@@H](CC)O5)O4)OC1=O)C)[C@@]23O)[H])[H].[C@]12([H])C=C(C)/C(=N\O)/[C@@]3([H])OCC(=CC=C[C@H](C)CC(C)=CC[C@]4([H])C[C@@]([H])(C[C@@]5(O4)CC[C@H](C)[C@@H](C)O5)OC1=O)[C@@]23O.[C@]12([H])C=C(C)/C(=N/O)/[C@@]3([H])OCC(=CC=C[C@H](C)CC(C)=CC[C@]4([H])C[C@@]([H])(C[C@@]5(O4)CC[C@H](C)[C@@H](C)O5)OC1=O)[C@@]23O |c:11,58,108,155,t:13,19,60,65,110,116,157,163,&1:0,7,15,22,25,28,31,33,41,44,51,58,64,67,70,73,75,84,88,96,104,111,114,117,121,123,129,131,139,147,154,157,160,164,166,172|
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| Synonyms |
CGA179246; CGA 179246; CGA-179246
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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 (~91.13 mM)
H2O : ~1 mg/mL (~0.91 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (2.28 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (1.90 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (1.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.9113 mL | 4.5563 mL | 9.1126 mL | |
| 5 mM | 0.1823 mL | 0.9113 mL | 1.8225 mL | |
| 10 mM | 0.0911 mL | 0.4556 mL | 0.9113 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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