Description
CGP 78608 hydrochloride is a highly potent and selective antagonist at the glycine-binding site of the NMDA receptor, with an IC50 of 6 nM. CGP 78608 acts as a potentiator of GluN1/GluN3A-mediated glycine currents, with an estimated EC50 in the low nM range (26.3 nM). Anticonvulsant activity.
Product information
CAS Number: 1135278-54-4
Molecular Weight: 414.58
Formula: C11H14BrClN3O5P
Chemical Name: [(1S)-1-{[(7-bromo-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)methyl]amino}ethyl]phosphonic acid hydrochloride
Smiles: Cl.C[C@@H](NCC1=CC(Br)=CC2NC(=O)C(=O)NC=21)P(O)(O)=O
InChiKey: MZQQZBPMRPDKTB-JEDNCBNOSA-N
InChi: InChI=1S/C11H13BrN3O5P.ClH/c1-5(21(18,19)20)13-4-6-2-7(12)3-8-9(6)15-11(17)10(16)14-8;/h2-3,5,13H,4H2,1H3,(H,14,16)(H,15,17)(H2,18,19,20);1H/t5-;/m0./s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
CGP-78608 hydrochloride decreases glycine sensitivity of GluN1/GluN3A receptors through an inter-subunit allosteric effect between GluN1 and GluN3A agonist-binding domain (ABD) sites. CGP 78608 hydrochloride reduces or abolishes ammonia-dependent cGMP synthesis which is a causative factor of ammonia neurotoxicity.
In Vivo:
CGP-78608 hydrochloride displays potent anticonvulsant effects after i.p. administration in the electroshock-induced convulsions assay in mice.
Products are for research use only. Not for human use.
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