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RPR104632

Catalog No. T16797   CAS 154106-92-0

RPR104632 is a novel and potent antagonist located at the NMDA glycine site with neuroprotective activity.

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RPR104632 Chemical Structure
RPR104632, CAS 154106-92-0
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1 mg In stock $ 700.00
5 mg In stock $ 1,800.00
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Purity: 99.06%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description RPR104632 is a novel and potent antagonist located at the NMDA glycine site with neuroprotective activity.
Targets&IC50 Cerebral cortex:4.9 nM (Ki,rat), Neuroprotection:4 μM (EC50), Neuro:4 μM (EC50), Cerebellar slices:890 nM (rat), [3H]-TCP:55 nM
In vitro RPR104632 antagonizes the binding of [3H]5,7-dichlorokynurenic acid to the rat cerebral cortex with a Ki of 4.9 nM. In the presence of N-methyl-D-aspartate (NMDA), RPR104632 inhibits [3H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine ([3H]TCP) binding with an IC50 of 55 nM. In a non-competitive manner, RPR104632 inhibits the NMDA-evoked increase in guanosine 3',5'-cyclic monophosphate (cGMP) levels of neonatal rat cerebellar slices (IC50 = 890 nM) and markedly reduces NMDA-induced neurotoxicity in rat hippocampal slices and cortical primary cell cultures. While MK-801 (1 μM) completely protects the CA1 and CA3 pyramidal neurones against NMDA-induced toxicity, these effects are not blocked by glycine. RPR104632 consistently produces a significant neuroprotective effect against all NMDA-induced toxicity and has no effect when added alone at concentrations up to 10 μM. The neuroprotective potency of RPR104632 is characterized by an EC50 of 4 μM[1].
Molecular Weight 466.13
Formula C15H11BrCl2N2O4S
CAS No. 154106-92-0

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

1. Boireau A, et al. Neuroprotective effects of RPR 104632, a novel antagonist at the glycine site of the NMDA receptor, in vitro. Eur J Pharmacol. 1996 Apr 11;300(3):237-46.

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Keywords

RPR104632 154106-92-0 Neuroscience NMDAR RPR 104632 RPR-104632 inhibitor inhibit

 

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