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CP-465022 (maleate) Sale

目录号 : GC12742

An AMPA receptor antagonist

CP-465022 (maleate) Chemical Structure

Cas No.:199656-46-7

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1mg
¥444.00
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5mg
¥1,301.00
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10mg
¥2,157.00
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Sample solution is provided at 25 µL, 10mM.

Description

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 [1].

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 [2].

Clinical trial: So far, no clinical study has been conducted.

References:
[1] Lazzaro JT, Paternain AV, Lerma J, Chenard BL, Ewing FE, Huang J, Welch WM, Ganong AH, Menniti FS.  Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist. Neuropharmacology. 2002 Feb;42(2):143-53.
[2] Menniti FS, Buchan AM, Chenard BL, Critchett DJ, Ganong AH, Guanowsky V, Seymour PA, Welch WM.  CP-465,022, a selective noncompetitive AMPA receptor antagonist, blocks AMPA receptors but is not neuroprotective in vivo. Stroke. 2003 Jan;34(1):171-6.

化学性质

Cas No. 199656-46-7 SDF
化学名 3-(2-chlorophenyl)-2-[2-[6-[(diethylamino)methyl]-2-pyridinyl]ethenyl]-6-fluoro-4(3H)-quinazolinone-(2Z)-2-butenedioate
Canonical SMILES FC1=CC=C2C(C(N(C3=C(Cl)C=CC=C3)C(/C=C/C4=CC=CC(CN(CC)CC)=N4)=N2)=O)=C1.OC(/C=C\C(O)=O)=O
分子式 C26H24ClFN4O • C4H4O4 分子量 579.0
溶解度 Soluble in DMSO 储存条件 Room temperature
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1 mg 5 mg 10 mg
1 mM 1.7271 mL 8.6356 mL 17.2712 mL
5 mM 0.3454 mL 1.7271 mL 3.4542 mL
10 mM 0.1727 mL 0.8636 mL 1.7271 mL
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