Fluxametamide
(Synonyms: 4-[5-(3,5-二氯苯基)-4,5-二氢-5-(三氟甲基)-3-异恶唑基]-N-[(甲氧基氨基)亚甲基]-2-甲基苯甲酰胺) 目录号 : GC30088
Fluxametamide是一种GABA和谷氨酸门控氯离子通道的拮抗剂，对GABACls和GluCls的IC50值分别为1.95nM和225nM。
Cas No.:928783-29-3
Sample solution is provided at 25 µL, 10mM.
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Fluxametamide is an antagonist of GABA- and Glu-gated chloride channels (GABACls and GluCls) with IC50 value of 1.95nM and 225nM, respectively[1]. Fluxametamide mainly bound in transmembrane domain (TM)3 domain by forming amide-pi stacked with Gly316, pi-alkyl with Val313, Leu315 and Phe319 [2]. Fluxametamide has been widely used as an insecticide, inhibiting the growth of various pests, including Lepidoptera, Acarina, Thysanoptera, and Diptera[3].
In vivo, Fluxametamide (dissolved in the water environment) has a relatively high toxicity to zebrafish with LC50=0.785mg/L after a 96-hour treatment[4].
References:
[1] Asahi M, Kobayashi M, Kagami T, et al. Fluxametamide: A novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels[J]. Pesticide biochemistry and physiology, 2018, 151: 67-72.
[2] Yin X, Li S, Tian Q, et al. Comparison of the toxicity and pharmacological effects of two insecticides against the Asian corn borer, Ostrinia furnacalis[J]. Pesticide Biochemistry and Physiology, 2025: 106597.
[3] Li R, Pan X, Wang Q, et al. Development of S-fluxametamide for bioactivity improvement and risk reduction: systemic evaluation of the novel insecticide fluxametamide at the enantiomeric level[J]. Environmental science & technology, 2019, 53(23): 13657-13665.
[4] Huang Q, Jia Z, Wu S, et al. The acute toxicity, mechanism, bioconcentration and elimination of fluxametamide on zebrafish (Danio rerio)[J]. Environmental Pollution, 2023, 317: 120808.
Fluxametamide是一种GABA和谷氨酸门控氯离子通道的拮抗剂，对GABACls和GluCls的IC50值分别为1.95nM和225nM[1]。Fluxametamide主要通过在跨膜域（TM3）中与Gly316形成酰胺-π堆积以及与Val313、Leu315和Phe319形成π-烷基堆积的方式进行结合[2]。Fluxametamide已作为杀虫剂广泛应用，可抑制包括鳞翅目、螨类、缨翅目和双翅目在内的多种害虫的生长[3]。
在体内，将Fluxametamide溶解于水环境中处理斑马鱼96小时，表现出相对较高的毒性，LC50值为0.785mg/L[4]。
| Animal experiment [1]: | |
Animal models | Zebrafish (Danio rerio) |
Preparation Method | 150 Zebrafish (Danio rerio) were placed in a water environment containing 0.0314mg/L of Fluxametamide, and were continuously raised for 32 days. Every day, 6 zebrafish and 0.8ml of water sample were taken from each working solution for bioaccumulation detection. |
Dosage form | 0.0314mg/L; 32 days; expose to water environment |
Applications | Fluxametamide showed high bioconcentration level in Zebrafish at 0.0314mg/L. |
References: | |
| Cas No. | 928783-29-3 | SDF | |
| 别名 | 4-[5-(3,5-二氯苯基)-4,5-二氢-5-(三氟甲基)-3-异恶唑基]-N-[(甲氧基氨基)亚甲基]-2-甲基苯甲酰胺 | ||
| Canonical SMILES | FC(F)(C1(C2=CC(Cl)=CC(Cl)=C2)CC(C3=CC(C)=C(C(N/C=N/OC)=O)C=C3)=NO1)F | ||
| 分子式 | C20H16Cl2F3N3O3 | 分子量 | 474.26 |
| 溶解度 | DMSO : 125 mg/mL (263.57 mM);Water : < 0.1 mg/mL (insoluble) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1085 mL | 10.5427 mL | 21.0855 mL |
| 5 mM | 421.7 μL | 2.1085 mL | 4.2171 mL |
| 10 mM | 210.9 μL | 1.0543 mL | 2.1085 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet