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RPR104632

SKU: orb1706686

Description

RPR104632 is a potent and selective antagonist of the NMDA receptor glycine site, exhibiting neuroprotective properties. It is a valuable research tool for studying excitotoxicity and neurodegeneration in both in vitro cellular models and in vivo animal studies of stroke and CNS injury.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number154106-92-0
MW466.13
Purity99.06% (May vary between batches)
FormulaC15H11BrCl2N2O4S
SMILESO=C(O)C1NC=2C=C(Cl)C=C(Cl)C2S(=O)(=O)N1CC=3C=CC=C(Br)C3
TargetNMDAR,iGluR

Bioactivity

Target IC50
Neuro:4 μM (EC50)|Cerebral cortex:4.9 nM (Ki,rat)|Cerebellar slices:890 nM (rat)|Neuroprotection:4 μM (EC50)|[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.

Storage & Handling

Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

NMDA, RPR104632, RPR-104632, RPR 104632
Quality Guarantee

Quality Guarantee

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Key Properties

No computed properties available.

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Protocol Information

RPR104632 (orb1706686)

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1 mg
$ 740.00
5 mg
$ 1,840.00
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