Doramectin

한글명:Doramectin

카스 번호117704-25-3

상품명:Doramectin

CBNumberCB4167857

분자식C50H74O14

포뮬러 무게899.11

MOL 파일117704-25-3.mol

화학적 성질

녹는점	116-1190C
끓는 점	967.4±65.0 °C(Predicted)
밀도	1.25±0.1 g/cm3(Predicted)
증기압	0Pa at 20℃
저장 조건	Sealed in dry,Store in freezer, under -20°C
용해도	메탄올 에 용해됨
물리적 상태	고체
물리적 상태	단단한 모양
산도 계수 (pKa)	12.42±0.70(Predicted)
색상	하얀색
InChIKey	QLFZZSKTJWDQOS-YDBLARSUSA-N
LogP	4.39-4.43 at 25℃

위험 및 안전 성명

위험품 표기

T,N,Xi

위험 카페고리 넘버

25-50/53-36/37/38

안전지침서

33-45-60-61-36/37-26

유엔번호(UN No.)

UN 2811 6.1/PG 3

WGK 독일

HS 번호

29419090

유해 물질 데이터

117704-25-3(Hazardous Substances Data)

NFPA 704:

	0
2		0

그림문자(GHS)

Doramectin MSDS

Doramectin 화학적 특성, 용도, 생산

개요
Doramectin[117704-25-3] is a novel avermectin with a cyclohexyl substituent on the previously inaccessible C-25 position of the molecule; the substitution was facilitated by mutational biosynthesis. The discovery of doramectin involved feeding carboxylic acids or their precursors to a fermentation of Streptomyces avermitilis that lacked branched-chain 2-oxo acid dehydrogenase activity, and then screening the resultant fermentation products for anthelmintic and ectoparasiticidal activity. Two dosage forms of doramectin have been developed for use as an endectocide on cattle, an injectable formulation for subcutaneous administration and a pouron formulation. An injectable formulation is also approved for use on pigs.
화학적 성질
White solid or slightly yellow-brown powder with poor water solubility, low stability, easily decomposed and deactivated by sunlight. The remaining drug residue is toxic to fish and aquatic organisms, requiring water source protection.
용도
Doramectin is a biosynthetic avermectin derived from a mutant strain of Streptomyces avermitilis, supplemented with a cyclohexylcaboxylic acid starting unit. Doramectin was developed as an anthelmintic for internal parasite control. The presence of the cyclohexyl group replacing the sec-butyl moiety affords greater hydrophobicity and longer biological half-life compared to avermectin. Like the other milbemycin/avermectins, it selectively binds to parasite glutamate-gated chloride ion channels and disrupts neurotransmission leading to paralysis and death of the parasite.
주요 응용
Doramectin is a mutational biosynthetic antiparasitic antibiotic structurally related to the avermectins. Avermectins are a group of agents that occurs naturally as a product of fermenting Streptomyces avermitilis, isolated from the soil. Avermectins are composed of a structurally similar 16-membered macrocyclic lactone, and widely used as insecticidal and antiparasitic agents. Doramectin is one of the best of a series of avermectins with antiparasitic activity.
Structure and conformation
Doramectin is a macrolide drug of the avermectin family, which is very similar in structure to ivermectin. Doramectin C25 is cyclohexane, and ivermectin is a mixture of several homologues. The C25 of its highly active component B1a (80%) is CH(CH3)C2H5, and the C25 of another component B1b (20%) is CH(CH3)-CH3. Doramectin has a double bond between C22 and C23, while ivermectin has a single bond.
참고 문헌
1. Production of doramectin by rational engineering of the avermectin biosynthetic pathway. DOI:10.1016/j.bmcl.2011.04.008
2. Construction of a doramectin producer mutant from an avermectin-overproducing industrial strain of Streptomyces avermitilis.DOI:10.1139/W09-098
3. An alternative derivatization reaction to the determination of doramectin in bovine milk using spectrofluorimetry.DOI:10.1016/j.saa.2012.02.084
4. Doramectin - a potent novel endectocide. DOI:10.1016/0304-4017(93)90218-C
5. Avermectin derivatives, pharmacokinetics, therapeutic and toxic dosages, mechanism of action, and their biological effects (a review). DOI:10.3390/ph13080196
6. Research progress of avermectin: A minireview based on the structural derivatization of avermectin. DOI:10.1016/j.aac.2022.11.001
7. Positive and negative electrospray LC-MS-MS methods for quantitation of the antiparasitic endectocide drugs, abamectin, doramectin, emamectin, eprinomectin, ivermectin, moxidectin and selamectin in milk. DOI:10.1016/J.JCHROMB.2006.11.014
8. https://www.fda.gov/animal-veterinary/cvm-updates/fda-approves-first-generic-doramectin-topical-solution-treatment-certain-parasites-cattle

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