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Merck
CN

SML4081

Lotilaner

≥98% (HPLC)

别名:

5-[(5S)-4,5-Dihydro-5-(3,4,5-trichlorophenyl)-5-(trifluoromethyl)-3-isoxazolyl]-3-methyl-N-[2-oxo-2-[(2,2,2-trifluoroethyl)amino]ethyl]-2-thiophenecarboxamide

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关于此项目

经验公式(希尔记法):
C20H14Cl3F6N3O3S
化学文摘社编号:
分子量:
596.76
MDL编号:
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质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

-10 to -25°C

SMILES字符串

FC(F)(F)[C@@]2(ONC(=C2)c3[s]c(c(c3)C)C(=O)NCC(=O)NCC(F)(F)F)c1cc(c(c(c1)Cl)Cl)Cl

InChI

1S/C20H14Cl3F6N3O3S/c1-8-2-13(36-16(8)17(34)30-6-14(33)31-7-19(24,25)26)12-5-18(35-32-12,20(27,28)29)9-3-10(21)15(23)11(22)4-9/h2-5,32H,6-7H2,1H3,(H,30,34)(H,31,33)/t18-/m0/s1

InChI key

DPFOXZCPAGCTER-SFHVURJKSA-N

生化/生理作用

Orally available and potent inhibitor of γ-aminobutyric acid (GABA)-gated chloride channels; parasiticide.
Lotilaner is an oral isooxazoline ectoparasitic veterinary medication used to control fleas and ticks in dogs and cats. Lotilaner, similarly to other isoxazolines, targets gamma-aminobutyric acid (GABA) receptors. It binds to the GABA-gated chloride channels in nerve and muscle cells, which blocks the transmission of neuronal signals and leads to paralysis and death.

象形图

Environment

警示用语:

Warning

危险声明

预防措施声明

危险分类

Aquatic Acute 1 - Aquatic Chronic 1

储存分类代码

11 - Combustible Solids

WGK

WGK 2

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

新产品
此项目有

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Omar Hashim et al.
Molecular pharmacology, 102(2), 116-127 (2022-07-21)
Human louse Pediculus humanus is a cosmopolitan obligatory blood-feeding ectoparasite causing pediculosis and transmitting many bacterial pathogens. Control of infestation is difficult due to the developed resistance to insecticides that mainly target GABA (γ-aminobutyric acid) receptors. Previous work showed that
The novel isoxazoline ectoparasiticide lotilaner (Credelio?): a non-competitive antagonist specific to invertebrates ?-aminobutyric acid-gated chloride channels (GABACls).
Parasites & vectors, 10(1), 530-530 (2017)
Ian Benjamin Gaddie et al.
Ophthalmology, 130(10), 1015-1023 (2023-06-08)
To evaluate the safety and efficacy of lotilaner ophthalmic solution 0.25% compared with vehicle for the treatment of Demodex blepharitis. Prospective, randomized, double-masked, vehicle-controlled, multicenter, phase 3 clinical trial. Four hundred twelve patients with Demodex blepharitis were assigned randomly in

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