RPR104632

RPR104632 is a specific antagonist of NMDA receptor, with potent neuroprotective properties.

Product information

CAS Number: 154106-92-0

Molecular Weight: 466.13

Formula: C15H11BrCl2N2O4S

Chemical Name: 2-[(3-bromophenyl)methyl]-6,8-dichloro-1,1-dioxo-3,4-dihydro-2H-1λ⁶,2,4-benzothiadiazine-3-carboxylic acid

Smiles: OC(=O)C1NC2=CC(Cl)=CC(Cl)=C2S(=O)(=O)N1CC1C=C(Br)C=CC=1

InChiKey: HNXXFIJGNAGRFN-UHFFFAOYSA-N

InChi: InChI=1S/C15H11BrCl2N2O4S/c16-9-3-1-2-8(4-9)7-20-14(15(21)22)19-12-6-10(17)5-11(18)13(12)25(20,23)24/h1-6,14,19H,7H2,(H,21,22)

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

How to use

In Vitro:

RPR104632 antagonizes the binding of [3H]5,7-dichlorokynurenic acid to the rat cerebral cortex, with a Ki of 4.9 nM. RPR104632 inhibits [3H]N-[1-(2-thienyl)cyclohexyl]-3,4-piperidine ([3H]TCP) binding in the presence of N-methyl-D-aspartate (NMDA) (IC50 = 55 nM). RPR104632 inhibits the NMDA-evoked increase in guanosine 3',5'-cyclic monophosphate (cGMP) levels of neonatal rat cerebellar slices (IC50 = 890 nM) in a non-competitive manner and markedly reduces NMDA-induced neurotoxicity in rat hippocampal slices and in cortical primary cell cultures. MK-801 (1 μM) completely protects the CA1 and CA3 pyramidal neurones against NMDA-induced toxicity, but these effects are not blocked by glycine. RPR104632 produces a significant and consistent neuroprotective effect towards all the NMDA-induced toxicity and has no effect when it is added alone at concentrations up to 10 μM. RPR104632 has neuroprotective potencies, with EC50 of 4 μM.

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