Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fluxametamide is a novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels, acts as an antagonist of GABA- and glutamate-gated chloride channels(IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
---|---|---|---|---|---|
サンプルについてお問い合わせ | |||||
1 mg | 在庫あり | ¥ 9,500 | |||
5 mg | 在庫あり | ¥ 22,500 | |||
10 mg | 在庫あり | ¥ 35,500 | |||
25 mg | 在庫あり | ¥ 67,500 | |||
50 mg | 在庫あり | ¥ 123,500 | |||
100 mg | 在庫あり | ¥ 176,500 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 22,500 |
説明 | Fluxametamide is a novel isoxazoline insecticide that acts via distinctive antagonism of insect ligand-gated chloride channels, acts as an antagonist of GABA- and glutamate-gated chloride channels(IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls). |
ターゲット&IC50 | GABACls (M. domestica):1.95 nM , GluCls (M. domestica):225 nM |
In vitro | Fluxametamide inhibits GABA responses in the wild-type L. striatellus GABACls with IC50 values of 1.40 (0.57-3.29) nM; in the A2′N mutant GABACls, the IC50 value is 3.51 (2.17-5.69) nM. Moreover, Fluxametamide scarcely inhibits GABA (EC50)-induced currents in rat GABACls at 10 μM and with no inhibition on glycine (EC50)-induced current in human α1 GlyCls at tested concentrations.Fluxametamide is an antagonist of GABA- and glutamate-gated chloride channels, dose-dependently inhibits currents induced by GABA and glutamate in M. domestica GABACls and GluCls, with IC50 values of 1.95 (1.18-3.21) nM and 225 (137-372) nM, respectively, and displays potent antagonistic activity against T. urticae GABACls with an IC50 of 0.219 (0.127-0.381) nM. |
In vivo | Fluxametamide exerts distinctive antagonism of arthropod GABACls by binding to a site different from those for existing antagonists.In contrast to its profound actions on the arthropod LGCCs, the antagonistic activity of fluxametamide against rat GABACls and human glycine-gated chloride channels was nearly insignificant, suggesting that fluxametamide has high target-site selectivity for arthropods over mammals.Overall, fluxametamide is a new type of LGCC antagonist insecticide with excellent safety for mammals at the target-site level. |
分子量 | 474.26 |
分子式 | C20H16Cl2F3N3O3 |
CAS No. | 928783-29-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 125 mg/mL (263.57 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
bottom
Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
Fluxametamide 928783-29-3 Membrane transporter/Ion channel Neuroscience GABA Receptor inhibit Inhibitor γ-Aminobutyric acid Receptor Gamma-aminobutyric acid Receptor inhibitor