Milbemycin Oxime

Synonyms: Milbemycin oxime, Milbemycin 5-oxime, A3/A4 oxime, Interceptor, Sentinel, 129496-10-2

Milbemycin oxime is a semi-synthetic macrocyclic lactone derived from the natural fermentation products of Streptomyces hygroscopicus var. aureolacrimosus. Structurally, it is a mixture of two homologous oxime derivatives, milbemycin A3 oxime and milbemycin A4 oxime, typically in a ratio of about 20:80. This molecule belongs to the milbemycin family, which shares mechanistic similarities with the avermectins but lacks the disaccharide substituent at C-13. The oxime modification at C-5 significantly enhances antiparasitic potency and extends the spectrum of activity compared to the parent milbemycins. First developed by Sankyo (now part of Mitsubishi Tanabe Pharma) and later marketed by Novartis, milbemycin oxime has become a mainstay in veterinary medicine for the prevention and treatment of a broad range of endo- and ectoparasites in dogs and cats.

In terms of chemical behavior, milbemycin oxime is a lipophilic compound that acts on glutamate-gated chloride channels in invertebrates, leading to hyperpolarization of nerve and muscle cells, paralysis, and eventual death of the parasite. Its selectivity for invertebrate channels over mammalian ones underpins its wide margin of safety. The A3 and A4 components differ by a single methylene group, which slightly affects their pharmacokinetic profiles but both contribute to the overall efficacy. The oxime group also improves stability and allows for formulation into chewable tablets, topical spot-ons, and injectables.

Commercially, milbemycin oxime is standardized to a minimum of 95% total oximes (A3 + A4) by HPLC, with individual component ratios controlled to ensure consistent biological performance. It is primarily used as an active pharmaceutical ingredient (API) in veterinary parasiticides, often in combination with other agents such as praziquantel or lufenuron to broaden the spectrum. The compound is also investigated for use in human medicine, though its main market remains animal health. Its effectiveness against heartworm (Dirofilaria immitis), roundworms, hookworms, and whipworms has made it a key component in monthly preventive products.

Function & Mechanism

• Glutamate-gated chloride channel activation: Binds to and opens these channels in invertebrate nerve and muscle cells, causing paralysis and death of parasites.
• Broad-spectrum antiparasitic activity: Effective against nematodes (roundworms, hookworms, whipworms) and arthropods (mites, lice) at low doses.
• Heartworm prevention: Interrupts the life cycle of Dirofilaria immitis by killing infective larvae before they mature.
• Selective toxicity: Low affinity for mammalian GABA receptors and glutamate-gated channels, resulting in a wide safety margin.
• Synergistic combinations: Often co-formulated with praziquantel for tapeworm coverage or with lufenuron for flea control.

Source & Standardization

• Source: Semi-synthetic derivative of milbemycins produced by fermentation of Streptomyces hygroscopicus var. aureolacrimosus.
• Extraction: Fermentation, isolation of milbemycin A3/A4, followed by oximation and purification.
• Standardization: ≥ 95.0% total milbemycin oximes (A3 + A4) by HPLC; typical A3:A4 ratio 20:80.
• Forms: Off-white to pale yellow crystalline powder.
• Applications: Veterinary parasiticides (chewables, spot-ons, injectables), research on anthelmintic resistance.

Quality Specifications (QC Tests)

Bulk Supply & Documentation

• Monthly capacity: 500 kg
• Lead time: 3-5 business days (stock items)
• Documentation: COA, MSDS, TDS, DMF available upon request
• Packaging: 1 kg, 5 kg, 25 kg fiber drums with double polyethylene liners

Frequently Asked Questions

What is the minimum order quantity (MOQ) for Milbemycin Oxime?

Our standard MOQ is 1 kg. For larger quantities, we offer competitive pricing and can accommodate custom packaging.

How long does delivery take?

For stock items, delivery is 3-5 business days after order confirmation. We ship from our warehouse and provide tracking information promptly.

Do you provide a Certificate of Analysis (COA) and samples?

Yes, we provide a COA for each batch. Samples are available upon request; please contact our sales team for sample arrangements. Documentation such as MSDS and TDS can be provided within 1-2 days.

Contact & Ordering Information

• Company: LyvBio Co., Ltd.
• Address: Room 5-0203, Courtyard 205, Lianhu District, Xi’an, Shaanxi, China
• Email: info@lyvbio.com
• Phone: +86-29-65816888

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