ENX-101
ENX-101 is an orally active (GABAA) receptor partial positive allosteric modulator (PAM). ENX-101 is selective to α2β2γ2L (EC50 = 0.76 nM), α2β3γ2L (EC50 = 0.61 nM), α3 (EC50 = 1.97 nM), α5 (EC50 = 0.85 nM) subunits of GABA receptor. ENX-101 possesses antiseizure activity in several animal models.
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- Formel: C19H12D9F2N7O2
- Molecular Weight:426.47
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
ENX-101 (0.01 nM-10 μM) potently enhances currents generated by GABA in receptors containing α2,α3,α5 subunits but causes negligible potentiation ofα1 subunit-containing receptors in Chinese hamster ovary (CHO) cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ENX-101 (1-100 mg/kg, p.o., a single dose 2 h prior to electrical stimulation) significantly inhibits the behavioral seizure response and reduces the mean afterdischarge duration in both amygdala and the cortex in a dose-dependent manner with amygdala kindled seizure rat model[1].
ENX-101 (0.075-100 mg/kg, p.o., a single dose) significantly reduces the overall spike-and-wave discharge (SWD) during the post-treatment observation period (10-130 min) in male Wistar Genetic Absence Epilepsy Rat from Strasbourg (GAERS) rats[1].
ENX-101 (10-100 mg/kg, p.o., a single dose) did not cause motor impairments at anti-seizure doses in rat models[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Amygdala kindled seizure rat model [1]
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Dosage:1 mg/kg, 6 mg/kg, 30 mg/kg, 100 mg/kg
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Administration:Oral gavage (p.o.)
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Result:Significantly reduced the mean seizure severity score by -1.8 (p < 0.01), -3.2 (p < 0.001), -3.8 (p < 0.01) respectively.
Reduced mean afterdischarge duration in the cortex (−30%, p < 0.01; −53%, p < 0.01; and −66%, p < 0.001) and amygdala −26% (p < 0.01), −46% (p < 0.01), and −64% (p < 0.001).
Showed greatest reductions in seizure severity score (-4.0) and afterdischarge duration in the cortex (−76%, p < 0.05) and in the amygdala (−78%) with 100 mg/kg but without significance.
Resulted in average plasma exposures of 191, 487, and 1102 ng/mL 2 h after dosing with 1, 6, 30 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Molecular Weight 426.47
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Formel C19H12D9F2N7O2
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SMILES
FC1=CC=C(F)C=C1C2=NN=C3N2N=C(OCC4=NC=NN4C)C(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])=C3.O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
ENX-101 Related Classifications
HY-173251S Related Classifications
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