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- CAS号:
864731-61-3
- 规格:
1mLx10mM(inDMSO)/1mg/5mg
| 规格: | 1mLx10mM(inDMSO) | 产品价格: | ¥334.0 |
|---|---|---|---|
| 规格: | 1mg | 产品价格: | ¥141.0 |
| 规格: | 5mg | 产品价格: | ¥289.0 |
Product Introduction
Bioactivity
| 名称 | Fluralaner |
| 描述 | Fluralaner (A1443) is an isoxazoline ectoparasiticide. It potently and selectively inhibits binding of the GABA receptor channel blocker EBOB to housefly head membranes (IC50: 455 pM). |
| 体外活性 | A1443通过抑制特定的伽马-氨基丁酸(GABA)受体通道阻断剂EBOB与苍蝇头膜的结合,表现出455pM的IC(50)值。相比之下,在大鼠脑膜中的IC(50)值>10muM。A1443还能阻断表达MdGBCl或MdGluCl通道的非洲爪蛙卵母细胞中,GABA和谷氨酸诱导的氯离子电流,其IC(50)值分别为5.32和79.9 nM [1]。Fluralaner显著抑制了体外跳蚤繁殖能力,仅在25.0 ng/mL的浓度下,产卵完全停止。虽然未观察到卵杀效果,但fluralaner在极低浓度(6.25 ng/mL)下展现了杀幼效果 [2]。 |
| 体内活性 | 在模拟的跳蚤滋生家庭环境中,对于接受fluralaner治疗的狗,跳蚤控制效果在12周内的每个测量时间点均超过99%。在接受fluralaner治疗的狗中没有观察到不良事件[2]。在以最高预期临床剂量的三倍治疗MDR1(-/-) Collies后,也没有观察到不良事件[3]。 |
| 存储条件 | Keep away from direct sunlight,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 4 mg/mL (7.19 mM), Sonication is recommended. DMSO : 250 mg/mL (449.41 mM), Sonication is recommended. H2O : Insoluble |
| 关键字 | Parasite | Inhibitor | inhibit | GABAReceptor | GABA Receptor | GABA | Fluralaner | AH-252723 | AH 252723 | A-1443 | A 1443 |
| 相关产品 | 2-Amino-2-methyl-1-propanol | Penicillin G sodium salt | p-Hydroxybenzaldehyde | Urethane | Fenpyroximate | Coumaran | Doxycycline | Metronidazole | Methylene Blue trihydrate | Hydroxychloroquine | Gum arabic | Kojic acid |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Approved Drug Library | Bioactive Compounds Library Max | EMA Approved Drug Library | Ion Channel Targeted Library | Membrane Protein-targeted Compound Library | Anti-Neurodegenerative Disease Compound Library | Anti-Parasitic Compound Library | Pain-Related Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library |
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¥141 - 334









