Milbemycin oxime
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MedKoo CAT#: 319518

CAS#: 129496-10-2 (oxime)

Description: Milbemycin oxime is a veterinary drug from the group of milbemycins, used as a broad spectrum antiparasitic. It is active against worms (anthelmintic), insects (insecticide) and mites (miticide). Milbemycin oxime is a semi-synthetic macrocyclic lactone prepared by the oxidation and oximation of an 80:20 ratio of milbemycin A3 and A. Like avermectins, milbemycins are products of fermentation by Streptomyces species. They have a similar mechanism of action, but a longer half-life than the avermectins. Milbemycin oxime is produced by Streptomyces hygroscopicus aureolacrimosus. It opens glutamate sensitive chloride channels in neurons and myocytes of invertebrates, leading to hyperpolarisation of these cells and blocking of signal transfer.

Chemical Structure

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Milbemycin oxime
CAS# 129496-10-2 (oxime)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 319518
Name: Milbemycin oxime
CAS#: 129496-10-2 (oxime)
Chemical Formula: N/A (mixture)
Exact Mass: 0.00
Molecular Weight: 0.000
Elemental Analysis: N/A (mixture)

Price and Availability

Size Price Availability Quantity
200mg USD 150 Ready to ship
500mg USD 250 Ready to ship
1g USD 450 Ready to ship
2g USD 750 Ready to ship
5g USD 1250 2 Weeks
10g USD 1950 2 Weeks
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Related CAS #: 51570-36-6 (free base)   129496-10-2 (oxime)   114177-14-9 (A3 Oxime)  

Synonym: CGA-179246; CGA 179246; CGA179246; Milbemycin A 5-oxime; Milbemite; Trifexis; Milbemycin oxime; trade name Interceptor.

IUPAC/Chemical Name: None (it is a mixture of two molecules)

InChi Key: CKVMAPHTVCTEMM-ALPQRHTBSA-N

InChi Code: InChI=1S/C32H45NO7.C31H43NO7/c1-6-27-21(4)12-13-31(40-27)17-25-16-24(39-31)11-10-20(3)14-19(2)8-7-9-23-18-37-29-28(33-36)22(5)15-26(30(34)38-25)32(23,29)35;1-18-7-6-8-23-17-36-28-27(32-35)21(4)14-26(31(23,28)34)29(33)37-25-15-24(10-9-19(2)13-18)39-30(16-25)12-11-20(3)22(5)38-30/h7-10,15,19,21,24-27,29,35-36H,6,11-14,16-18H2,1-5H3;6-9,14,18,20,22,24-26,28,34-35H,10-13,15-17H2,1-5H3/b8-7+,20-10+,23-9+,33-28-;7-6+,19-9+,23-8+,32-27-/t19-,21-,24+,25-,26-,27+,29+,31+,32+;18-,20-,22+,24+,25-,26-,28+,30-,31+/m00/s1

SMILES Code: CC[C@@H]1[C@H](CC[C@@]2(O1)C[C@@H]3C[C@H](O2)C/C=C(/C[C@H](/C=C/C=C/4\CO[C@H]\5[C@@]4([C@@H](C=C(/C5=N/O)C)C(=O)O3)O)C)\C)C.C[C@H]1CC[C@]2(C[C@@H]3C[C@H](O2)C/C=C(/C[C@H](/C=C/C=C/4\CO[C@H]\5[C@@]4([C@@H](C=C(/C5=N/O)C)C(=O)O3)O)C)\C)O[C@@H]1C

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target: Milbemycin oxime is a macrocyclic lactone that has broad-spectrum anti-parasitic activity and activity against intestinal nematodes, pulmonary, and cardiac helminths.
In vitro activity: TBD
In vivo activity: Dogs treated with Interceptor or Sentinel received a mean milbemycin oxime dose of 0.57 ± 0.08 and 0.57 ± 0.05 mg/kg, respectively. All dogs were reported as being over 10 months of age and the weight ranged from 4.7 to 21.3 kg two days prior to dosing (weight used to determine dose). There were no significant differences in body weights between treatment groups. Of the 12 dogs in the placebo control group, seven had more than 20 A. braziliense isolated at necropsy and 10 had more than five isolated at necropsy (range 10–100) indicating the presence of an adequate infection in the study dogs. Statistically, both milbemycin treatment groups had significantly (p < 0.0001) fewer A. braziliense isolated at necropsy when compared to the placebo control group. No adverse events were reported nor were there any significant reductions in body weight observed indicating milbemycin oxime in these formulations was well tolerated. Reference: Vet Parasitol. 2013 Jul 1;195(1-2):102-5. https://pubmed.ncbi.nlm.nih.gov/23375194/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100.0 91.13

Preparing Stock Solutions

The following data is based on the product molecular weight 0.00 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Bienhoff SE, Kok DJ, Roycroft LM, Roberts ES. Efficacy of a single oral administration of milbemycin oxime against natural infections of Ancylostoma braziliense in dogs. Vet Parasitol. 2013 Jul 1;195(1-2):102-5. doi: 10.1016/j.vetpar.2013.01.004. Epub 2013 Jan 16. PMID: 23375194
In vitro protocol: TBD
In vivo protocol: 1. Bienhoff SE, Kok DJ, Roycroft LM, Roberts ES. Efficacy of a single oral administration of milbemycin oxime against natural infections of Ancylostoma braziliense in dogs. Vet Parasitol. 2013 Jul 1;195(1-2):102-5. doi: 10.1016/j.vetpar.2013.01.004. Epub 2013 Jan 16. PMID: 23375194.

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