Description Uses Drug Interactions Uses Mechanism of action Side Effects
ChemicalBook > CAS DataBase List > Milbemycin oxime

Milbemycin oxime

Description Uses Drug Interactions Uses Mechanism of action Side Effects
Product Name
Milbemycin oxime
CAS No.
129496-10-2
Chemical Name
Milbemycin oxime
Synonyms
Milbemite;Mibemycin oxime;Milbemycin oxime;Milbemycin oxime CRS;β-phenylacrylophenone;Milbemycin Oxime (200 mg);Milbemycin Oxime (1443806);Sodium Pyrithione 3811-73-2;Milbemycin, oxime (9CI, ACI);Milbemycin Oxime (Mixture of Milbemycin Oxime A3 and A4)
CBNumber
CB11104418
Molecular Formula
2C32H45NO7.2C31H43NO7
Formula Weight
2194.78
MOL File
129496-10-2.mol
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Milbemycin oxime Property

Melting point:
169.6-177.4°
Flash point:
412℃
storage temp. 
Store at -20°C
solubility 
DMSO:100.0(Max Conc. mg/mL);91.13(Max Conc. mM)
form 
A crystalline solid
Stability:
Hygroscopic
InChIKey
LKMMLHTWKLEARD-MGZQXKBQSA-N
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Safety

RIDADR 
2588
WGK Germany 
3
HazardClass 
6.1(b)
PackingGroup 
III
HS Code 
2932206000
Toxicity
LD50 orally in mice: 1000-1500 mg/kg (Ciba-Geigy)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H410Very toxic to aquatic life with long lasting effects

Precautionary statements

P273Avoid release to the environment.

P391Collect spillage. Hazardous to the aquatic environment

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
PHR2633
Product name
Milbemycin oxime
Purity
Pharmaceutical Secondary Standard; Certified Reference Material, certified reference material, pharmaceutical secondary standard, pkg of 500?mg
Packaging
500MG
Price
$267
Updated
2024/03/01
Sigma-Aldrich
Product number
1443806
Product name
Milbemycin oxime
Packaging
200mg
Price
$436
Updated
2024/03/01
Cayman Chemical
Product number
17164
Product name
Milbemycin oxime
Purity
≥95%
Packaging
5mg
Price
$32
Updated
2024/03/01
Cayman Chemical
Product number
17164
Product name
Milbemycin oxime
Purity
≥95%
Packaging
10mg
Price
$48
Updated
2024/03/01
Cayman Chemical
Product number
17164
Product name
Milbemycin oxime
Purity
≥95%
Packaging
50mg
Price
$139
Updated
2024/03/01
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Milbemycin oxime Chemical Properties,Usage,Production

Description

Milbemycin is an oral medication used as a dewormer and heartworm preventive. This medication should not be used in doses higher than the recommended heartworm prevention dose, except under veterinary supervision. Studies support the safety of milbemycin products in Collies and other breeds prone to the MDR-1 gene mutation when used at the recommended heartworm prevention dose.

Uses

Milbemycin Oxime is active against a broad spectrum of nematodes, although it is less potent against heartworms than ivermectin. Its miticide spectrum includes Sarcoptes and Demodex. The USA FDA approval for milbemycin oxime as formulated alone does not indicate insecticidal activity. The substance is often combined with other parasiticides to achieve a broader spectrum of action. Such products include: Milbemax (with praziquantel) Sentinel Flavor Tabs (with lufenuron) Recently the drug has been used in marine reef aquaria to control parasitic harptacoid copepod (Tegastidae) infestations on captive hard coral colonies. It is an effective full tank treatment for these parasites because it is not toxic to corals in the dosage required to kill the parasites. Shrimps, crabs and other crustaceans should be removed prior to treatment, as they will be killed by the treatment.

Drug Interactions

Milbemycin should not used in combination with cyclosporine, quinidine or ketoconazole.

Uses

Intestinal parasite deworming in dogs and for heartworm prevention in dogs and cats.

Mechanism of action

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.

Side Effects

The drug is tolerated well, even by dogs with multiple drug resistance. In high doses, it can cause side effects like stupor, tremor and ataxia.

Uses

Milbemycin oxime is a semi-synthetic macrocyclic lactone prepared by the oxidation and oximation of a mixture of two natural products, milbemycin A3 and A4 (in ~30:70 ratio). Milbemycin oxime is used therapeutically for the prevention of intestinal parasites in dogs. Like the other milbemycin/avermectins, it was developed for intestinal parasite control in animals and acts by opening glutamate sensitive chloride channels in neurons of invertebrates leading to paralysis by hyperpolarisation of these cells and signal transfer blocking.

Uses

controls intestinal parasites in animals

Clinical Use

Milbemycin oxime (Milbemycin) is available as an oral chewable tablet (2.3–27 mg) for heartworm prevention in dogs and cats, as well as a 0.1% otic solution for treating ear mites. It is not available in a more concentrated dosage form, so overdoses are relatively rare[1].

Toxicology

The therapeutic dosages of Milbemycin oxime (milbemycin) for heartworm prevention are 0.5 mg/kg in dogs and 2 mg/kg in cats. Mild clinical signs of ataxia, hypersalivation, mydriasis, and lethargy have been documented in ivermectin-sensitive dogs dosed at 5 to 10 mg/kg. In a separate report, two ABCB1-defective dogs developed mild signs (ataxia) after being dosed repeatedly with milbemycin for demodicosis; one dog received 0.8 mg/kg 2 days in a row, and the other dog received 1.5 mg/kg daily for 13 days before developing signs. Mild clinical signs have been reported to develop in normal dogs at 10 to 20 mg/kg and in cats and dogs with suspected ABCB1 gene deletions greater than 5 to 10 mg/kg. The most common clinical signs reported include ataxia, tremors, lethargy, vomiting, mydriasis, disorientation, and hypersalivation[1].

Veterinary Drugs and Treatments

Milbemycin tablets are labeled as a once-a-month heartworm preventative (Dirofilaria immitis) and for hookworm control (Ancylostoma caninum). It has activity against a variety of other parasites, including adult hookworms (A. caninum), adult roundworms (T. canis, T. leonina) and whipworms (Trichuris vulpis). In cats, milbemycin has been used successfully to prevent larval infection of Dirofilaria immitis.
Milbemycin, like ivermectin can be used for treatment of generalized demodicosis in dogs, but treatment can be significantly more expensive. It is likely safer to use in breeds susceptible to mdr1 genetic mutation (Collies, Shelties, Australian shepherds, etc.) at the doses used for this indication, but neuro toxicity is possible. Older dogs, those that have had a long duration of disease prior to treatment, and dogs with pododemodicosis appear have a lower success rate with milbemycin treatment.

References

[1] DVM, Valentina M. Merola, Paul A. Eubig DVM MS and MS. “Toxicology of Avermectins and Milbemycins (Macrocylic Lactones) and the Role of P-Glycoprotein in Dogs and Cats.” Veterinary Clinics of North America-Small Animal Practice 42 2 (2012): Pages 313-333.

Milbemycin oxime Preparation Products And Raw materials

Raw materials

Preparation Products

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Milbemycin oxime Suppliers

Taizhou Crene Biotechnology Co. Ltd.
Tel
0576-88813233 13396860566
Email
sales@pharm-intermediates.com
Country
China
ProdList
2013
Advantage
58
Wuhan Wiseman Bioengineering Co.,Ltd
Tel
027-59506022 13419526507
Fax
027-59506022
Email
13419526507@163.com
Country
China
ProdList
2935
Advantage
58
Shanghai Gukang Biotechnology Co., LTD
Tel
021-34080528 13564510648
Fax
021-54301252
Email
info@kanghaopharm.com
Country
China
ProdList
123
Advantage
58
Huzhou fuhe Rui biological medicine co., ltd
Tel
13626726938
Email
953022190@qq.com
Country
China
ProdList
791
Advantage
58
Jinan Hongkangda Chemical Co., Ltd
Tel
0531-0531-88901705 18753193522
Email
810353473@qq.com
Country
China
ProdList
137
Advantage
58
Guangzhou Reullei Pharmaceutical Technology Co., Ltd,
Tel
18664855715
Email
lx@reullei.com
Country
China
ProdList
299
Advantage
58
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2923
Advantage
55
Sinopharm Chemical Reagent Co,Ltd.
Tel
86-21-63210123
Fax
86-21-63290778 86-21-63218885
Email
sj_scrc@sinopharm.com
Country
China
ProdList
9823
Advantage
79
Wuhan Fortuna Chemical Co., Ltd
Tel
027-027-59207852 13308628970
Fax
QQ3130921841
Email
buy@fortunachem.com
Country
China
ProdList
2893
Advantage
58
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
sales@meilune.com
Country
China
ProdList
4647
Advantage
58
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View Lastest Price from Milbemycin oxime manufacturers

Shaanxi Haibo Biotechnology Co., Ltd
Product
Milbemycin oxime 129496-10-2
Price
US $0.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
2000ton
Release date
2023-09-06
airuikechemical co., ltd.
Product
milbemycin Oxime 129496-10-2
Price
US $0.00-0.00/kg
Min. Order
1kg
Purity
99.99%
Supply Ability
20 tons
Release date
2024-04-09
Shanghai Chinqesen Biotechnology Co., Ltd.
Product
Milbemycin oxime 129496-10-2
Price
US $30.00-20.00/kg
Min. Order
1kg
Purity
99%
Supply Ability
2000000
Release date
2023-10-30

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