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Cat. No.: HY-156505A

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R-(+)-EU-1180-453

R-(+)-EU-1180-453 is a positive allosteric modulator targeting NMDA receptors containing GluN2C and GluN2D subunits, with a pEC₅₀ value of 5.5 for both rat receptor subtypes, and it can cross the blood-brain barrier. R-(+)-EU-1180-453 increases the potency of glutamate, enhances receptor responses to maximally effective concentrations of agonists, and acts only on receptors bound to both co-agonists. R-(+)-EU-1180-453 is applicable to research related to Alzheimer's disease, Parkinson's disease, epilepsy, and neuropathic pain.

For research use only. We do not sell to patients.

CAS No.: 2488764-06-1
Formula: C₂₂H₂₁FN₂O₃
Molecular Weight:380.42

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Please store the product under the recommended conditions in the Certificate of Analysis.

R-(+)-EU-1180-453 Chemical Structure

CAS No.: 2488764-06-1

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Biological Activity

Description

All iGluR Isoforms :

In Vitro

R-(+)-EU-1180-453 (30 μM; concentrations for concentration−effect curves) potentiates GluN1/GluN2C and GluN1/GluN2D NMDA receptors expressed in Xenopus laevis oocytes with a pEC₅₀ of 5.5, maximal potentiation of 410% and 390% respectively, and a p(doubling concentration) of 5.9 and 5.8 respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

EU-1180-453 (10 mg/kg; i.p.; single dose) is brain-penetrant in male C57BL/6 mice, achieving a brain:plasma AUC_0-t ratio of 1.4 ± 0.5 after a single 10 mg/kg i.p. dose, with a plasma half-life of 1.07 ± 0.04 hours^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2488764-06-1
Molecular Weight 380.42
Formula C₂₂H₂₁FN₂O₃
SMILES

C(OC1=CC=C(OC)C=C1)[C@H]2C=3N(CC(=O)N2CC4=CC(F)=CC=C4)C=CC3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Epplin MP, et al. Discovery of Dihydropyrrolo[1,2-a]pyrazin-3(4H)-one-Based Second-Generation GluN2C- and GluN2D-Selective Positive Allosteric Modulators (PAMs) of the N-Methyl-d-Aspartate (NMDA) Receptor. J Med Chem. 2020;63(14):7569-7600. [Content Brief]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
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R-(+)-EU-1180-453

All iGluR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

R-(+)-EU-1180-453 Related Classifications

HY-156505A Related Classifications