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RPR104632

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Catalog No. T16797Cas No. 154106-92-0

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

RPR104632

RPR104632

😃Good
Purity: 99.06%
Catalog No. T16797Cas No. 154106-92-0
RPR104632 is a novel and potent antagonist located at the NMDA glycine site with neuroprotective activity.
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1 mg$7006-8 weeks
5 mg$1,8006-8 weeks
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Purity:99.06%
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Product Introduction

Bioactivity
Description
RPR104632 is a novel and potent antagonist located at the NMDA glycine site with neuroprotective activity.
Targets&IC50
Neuro:4 μM (EC50), [3H]-TCP:55 nM, Neuroprotection:4 μM (EC50), Cerebellar slices:890 nM (rat), Cerebral cortex:4.9 nM (Ki,rat)
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].
Chemical Properties
Molecular Weight466.13
FormulaC15H11BrCl2N2O4S
Cas No.154106-92-0
SmilesO=C(O)C1NC=2C=C(Cl)C=C(Cl)C2S(=O)(=O)N1CC=3C=CC=C(Br)C3
Relative Density.1.788g/cm3
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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