Moxidectin 113507-06-5

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Product Information

Product name	Moxidectin
CAS No.	113507-06-5
Molecular Formula	C₃₇H₅₃NO₈
Molecular Weight	639.83
Quality Standard	EP/USP
Appearance	White or pale yellow amorphous powder

COA

Test Items		Specifications	Results
Appearance		White or pale yellow amorphous powder.	White amorphous powder
Solubility(EP)		Practically insoluble in water, very soluble in ethanol(96%), slightly soluble in hexane.	Comply
Identification		IR spectrum of sample corresponds to that of reference substance.	Comply
Identification		The retention time of the major peak of the Sample solution corresponds to that of Standard solution, as obtained in the assay(USP).	Comply
Appearance of solution(EP)		The solution is clear and not more intensely coloured than reference solution GY5.	Comply
Water		≤1.3%	0.71%
Residue on ignition		≤0.2%	0.07%
Heavy metals		≤20ppm	<20ppm
Assay(USP)		Anhydrous basis 92.0%~102.0%	94.5%
Assay(EP)		Anhydrous basis 92.0%~102.0%	94.6%
Organic impurities	Early-eluting impurities	Moxidectin butenyl analog (A) ≤1.5%	0.36%
		5’-Demethyl moxidectin (B) ≤0.5%	0.20%
		Moxidectin pentenyl analog (C) ≤1.5%	0.39%
		Moxidectin 17a-epimer (D) ≤2.5%	Not detected
		Sum of moxidectin 19-S-17a-ene and moxidectin ethyl isomers (E+F) ≤1.7%	1.3%
		Milbemycin B analog (moxidectin open ring) (G) ≤1.5%	0.15%
		Any other individual impurity eluting before milbemycin B analog (moxidectin open ring) ≤0.5%	0.19%
	Late-eluting impurities	Moxidectin deoxydienea, and 4’-Methylthiomethoxymoxidectin (H+L) ≤0.5%	0.01%
		20b-Methylthiomoxidectin (J) ≤0.5%	Not detected
		20-Nitrobenzoylmoxidectin (K) ≤0.5%	Not detected
		Any other individual impurity eluting after the milbemycin B analog (moxidectin open ring) ≤0.5%	0.25%
	Total organic impurities	≤7.0%	3.4%
Solvent residue		Methanol ≤3000ppm	Not detected
		Methylene chloride ≤300ppm	Not detected
		Isopropyl acetate ≤5000ppm	Not detected
		N-heptane ≤5000ppm	106ppm
BHT		0.3%~0.6%	0.49%
Conclusion		The product complies with the specification (USP / EP).
Storage		Preserve in well-closed, light-resistant containers, and store in room temperature.

Usage

Moxidectin is a macrocyclic lactone endectocide and a semisynthetic derivative of nemadectin (produced by fermentation of Streptomyces cyano-griseus). As a potent anthelmintic and antiparasitic agent, it is widely used for the prevention and control of heartworm (Dirofilaria immitis) and intestinal worms in animals.

The mode of action of Moxidectin involves selectively binding to the glutamate-gated chloride ion channels in the nerve and muscle cells of invertebrates. This binding disrupts neurotransmission, leading to paralysis and death of the parasite, thereby effectively controlling infections. Compared to other macrocyclic lactones like ivermectin, Moxidectin exhibits greater lipophilicity, a longer half-life, and a more prolonged efficacy. Clinical trials have shown that Moxidectin clears microfilariae from the skin for a significantly longer time (up to one year) than ivermectin, making it particularly valuable in mass drug administration for diseases like onchocerciasis.

Moxidectin is effective against a broad spectrum of parasites, including gastrointestinal roundworms, lungworms, mites, and lice in various animals such as cattle, sheep, horses, dogs, and cats . It is also a substrate of BCRP and P-glycoprotein (P-gp), which influences its secretion into breast milk and its residue profile . Formulations containing Moxidectin are available for oral, subcutaneous, and topical administration.