CAS NO: | 951650-22-9 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
Molecular Weight (MW) | 353.42 |
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Formula | C23H19N3O |
CAS No. | 951650-22-9 |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO: ≥ 43 mg/mL |
Water: <1 mg/mL | |
Ethanol: <1 mg/mL | |
SMILES Code | N#CC1=CC=CC=C1C2=CC=CC(N3C4=CC=C(C(C)(O)C)C=C4N=C3)=C2 |
Synonyms | NS-11394; NS 11394; NS11394 |
In Vitro | In vitro activity: NS11394 is unique in having superior efficacy at GABA(A)-alpha(3) receptors while maintaining low efficacy at GABA(A)-alpha(1) receptors. NS11394 has an excellent pharmacokinetic profile, which correlates with pharmacodynamic endpoints (CNS receptor occupancy), yielding a high level of confidence in deriving in vivo conclusions anchored to an in vitro selectivity profile and allowing for translation to higher species Kinase Assay: NS11394 is a potent and subtype-selective GABA(A) receptor-positive modulator; possesses a functional efficacy selectivity profile of alpha(5)> alpha(3)> alpha(2)> alpha(1) at GABA(A) alpha subunit-containing receptors. Cell Assay: |
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In Vivo | Oral administration of NS11394 (1-30 mg/kg) to rats attenuated spontaneous nociceptive behaviors in response to hindpaw injection of formalin and capsaicin, effects that were blocked by the benzodiazepine site antagonist flumazenil |
Animal model | Mice |
Formulation & Dosage | 1-30 mg/kg; i.v. and p.o. |
References | J Pharmacol Exp Ther. 2008 Dec;327(3):969-81.J Pharmacol Exp Ther. 2008 Dec;327(3):954-68. |