氟雷拉纳 T5330

Product Introduction
Bioactivity


英文名: Fluralaner

描述: Fluralaner (A1443) 是一种异恶唑啉杀外寄生虫剂。 它有效且选择性地抑制 GABA 受体通道阻滞剂 EBOB 与家蝇头膜的结合，IC50值为 455 pM。

体外活性: A1443 inhibits specific binding of the gamma-aminobutyric acid (GABA) receptor channel blocker EBOB to housefly-head membranes, with an IC(50) value of 455pM. In contrast, the IC(50) value in rat-brain membranes is>10muM. A1443 blocks GABA- and glutamate-induced chloride currents in Xenopus oocytes expressing MdGBCl or MdGluCl channels, with IC(50) values of 5.32 and 79.9 nM, respectively [1]. Fluralaner potently inhibited flea reproduction capacity in vitro. Oviposition ceased completely at concentrations as low as 25.0 ng/mL. While no ovicidal effect was observed, fluralaner exerted a larvicidal effect at exceptionally low concentrations (6.25 ng/mL) [2].

体内活性: In the simulated flea-infested home environment, flea-control efficacy on fluralaner-treated dogs was >99% at every time point measured for 12 weeks. No adverse events were observed in fluralaner-treated dogs [2]. No adverse events were observed subsequent to fluralaner treatment of MDR1(-/-) Collies at three times the highest expected clinical dose [3].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 100 mg/mL (179.76 mM)
H2O : Insoluble


关键字: A-1443 | Parasite | inhibit | Fluralaner | AH-252723 | A 1443 | AH 252723 | Inhibitor

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相关库: Drug Repurposing Compound Library | Anti-Neurodegenerative Disease Compound Library | Neurotransmitter Receptor Compound Library | FDA-Approved & Pharmacopeia Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Anti-Parasitic Compound Library | Anti-Cancer Approved Drug Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途