RO 15-4513 CAS: 91917-65-6
MF: C15H14N6O3
MW: 326.31
A high affinty benzodiazepine ligand and GABAA antagonist.

RO 15-4513 (CAS 91917-65-6)

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Nomi alternativi: 8-Azido-5,6-dihydro-5-methyl-6-oxo-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylic acid ethyl ester
Applicazione: RO 15-4513 is a high affinty benzodiazepine ligand and GABAA antagonist
Numero CAS: 91917-65-6
Peso molecolare: 326.31
Formula molecolare: C15H14N6O3
Solo per uso in Ricerca. Non previsto per Uso Diagnostico o Terapeutico.
* Vedere Certificato di Analisi per informazioni sul lotto specifico (incluso il contenuto d'acqua).

RO 15-4513 is a high affinity benzodiazepine ligand which acts as a partial inverse agonist at recombinant diazepam-sensitive (DS) benzodiazepine α1-, α2-, α3- and α5-GABAA receptors. It has also been shown to activate GABAA R α4 and GABAA R α6. In addition, RO 15-4513 acts as a partial agonist at diazepam-insensitive (DI) benzodiazepine receptors. Furthermore, studies show that ethanol can inhibit the binding of RO 15-4513 to α4/6β3δ GABAA receptors. RO 15-4513 has a similar structure to flumazenil, which differs by an azido group at the C7 position of the imidazo-benzodiazepine ring.


Referenze

1. Turner, D.M., et al. 1991. J. Pharmacol. Exp. Ther. 257: 1236-1242. PMID: 1646328
2. Wong, G. and Skolnick, P. 1992. Eur. J. Pharmacol. 225: 63-68. PMID: 1311690
3. Hanchar, H.J., et al. 2006. Proc. Natl. Acad. Sci. U.S.A. 103: 8546-8551. PMID: 16581914

Stato fisico :
Solid
Solubilità :
Soluble in ethanol (5 mM), DMSO (10 mM), methanol, and 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin (0.8 mg/ml). Insoluble in water.
CONSERVAZIONE :
Desiccate at 4° C
Punto di scioglimento :
204-205° C
Punto di ebollizione :
701.35° C (Predicted)
IC50 :
GABAA Rα1: EC5050 = 1.1 nM (human)
Ki Data :
GABA-A receptor; alpha-5/beta-3/gamma-2: Ki= 0.27 nM (human); Diazepam-insensitive benzodiazepine receptors: Ki= 3.1 nM; GABAA Rα5: Ki= 3.1 nM (human); GABA-A receptor; anion channel: Ki= 3.1 nM (rat); Diazepam-sensitive benzodiazepine receptors: Ki= 5.3 nM
Valori pK :
pKb: 0.81 (Predicted)
Solo per uso in Ricerca. Non previsto per Uso Diagnostico o Terapeutico.
WGK Germania :
3
RTECS :
NI2922155
PubChem CID :
Numero MDL :
MFCD00078598
SMILES :
CCOC(=O)C1=C2CN(C(=O)C3=C(N2C=N1)C=CC(=C3)N=[N+]=[N-])C

Download SDS (MSDS)

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