CP-465022 (maleate)

IC50: 25 nM for AMPA receptor-mediated currents in rat cortical neurons CP-465022 is an AMPA antagonist. The inhibition of alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor has been hypothesized to lead to neuroprotective efficacy after cerebral ischemia on the basis of the activity in ischemia models of a variety of compounds with varying selectivity for AMPA over other glutamate receptor subtypes. In vitro: CP-465022 inhibited AMPA receptor-mediated currents in rat cortical neurons and such inhibition was found to be noncompetitive with agonist concentration. CP-465022 was selective for AMPA over kainate and N-methyl-D-aspartate receptors. However, CP-465022 was found to be equipotent for AMPA receptors composed of different AMPA receptor subunit combinations, which indicated that CP-465022 is equivalently potent for inhibition of AMPA receptor-mediated responses in different types of neurons expressing different AMPA receptor subunits . In vivo: Animal study showed that CP-465022 could potently and efficaciously inhibit AMPA receptor-mediated hippocampal synaptic transmission and the induction of seizures. However, at comparable doses, CP-465022 failed to prevent CA1 neuron loss after brief global ischemia or to reduce infarct volume after temporary middle cerebral artery occlusion . Clinical trial: So far, no clinical study has been conducted.

Product information

CAS Number: 199656-46-7

Molecular Weight: 579.02

Formula: C30H28ClFN4O5

Chemical Name: (2Z)-but-2-enedioic acid; 3-(2-chlorophenyl)-2-[(E)-2-{6-[(diethylamino)methyl]pyridin-2-yl}ethenyl]-6-fluoro-3,4-dihydroquinazolin-4-one

Smiles: CCN(CC1C=CC=C(/C=C/C2=NC3=CC=C(F)C=C3C(=O)N2C2C=CC=CC=2Cl)N=1)CC.OC(=O)/C=C\C(O)=O

InChiKey: WLLUWLRVXIHECY-KSUUAYPFSA-N

InChi: InChI=1S/C26H24ClFN4O.C4H4O4/c1-3-31(4-2)17-20-9-7-8-19(29-20)13-15-25-30-23-14-12-18(28)16-21(23)26(33)32(25)24-11-6-5-10-22(24)27;5-3(6)1-2-4(7)8/h5-16H,3-4,17H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b15-13+;2-1-

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

Products are for research use only. Not for human use.