928783-29-3
928783-29-3 structure
- Name: Fluxametamide
- Chemical Name: fluxametamide
- CAS Number: 928783-29-3
- Molecular Formula: C20H16Cl2F3N3O3
- Molecular Weight: 474.26100
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel Chloride Channel
- Create Date: 2017-09-06 03:38:43
- Modify Date: 2024-01-02 21:59:28
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Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls.
| Name | fluxametamide |
|---|---|
| Synonyms |
4-[(5RS)-5-(3,5-dichlorophenyl)-4,5-dihydro-5-(trifluoromethyl)-1,2-oxazol-3-yl]-N-[(EZ)-(methoxyimino)methyl]-o-toluamide
4-[5-(3,5-dichlorophenyl)-4,5-dihydro-5-(trifluoromethyl)-3-isoxazolyl]-N-[(methoxyamino)methylene]-2-methylbenzamide |
| Description | Fluxametamide is an insecticide with wide spectrum, acts as an antagonist of GABA- and glutamate-gated chloride channels, with IC50 of 1.95 nM and 225 nM for M. domestica GABACls and GluCls. |
|---|---|
| Related Catalog | |
| Target |
IC50: 1.95 nM (M. domestica GABACls), 225 nM (M. domestica GluCls)[1] |
| In Vitro | 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. 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[1]. |
| In Vivo | Fluxametamide shows significant insecticidal activity with an LD50 (LD95) value of 12.9 ± 4.9 ng/fly (38.7 ± 6.3 ng/fly)[1]. |
| References |
| Molecular Formula | C20H16Cl2F3N3O3 |
|---|---|
| Molecular Weight | 474.26100 |
| Exact Mass | 473.05200 |
| PSA | 72.28000 |
| LogP | 5.03000 |
| Storage condition | 2-8℃ |