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Radiprodil

Catalog No. T5385 CAS 496054-87-6

Synonyms: RGH-896

Radiprodil (RGH-896) (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).

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Radiprodil, CAS 496054-87-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 59.00
5 mg	In stock	$ 97.00
10 mg	In stock	$ 155.00
25 mg	In stock	$ 253.00
50 mg	In stock	$ 372.00
100 mg	In stock	$ 559.00
1 mL * 10 mM (in DMSO)	In stock	$ 97.00

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Purity: 99.9%

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Description	Radiprodil (RGH-896) (RGH-896) is an orally active and selective NMDA NR2B receptors antagonist. It was a potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP).
Targets&IC50	NR2B:69 nM
In vitro	The inhibition potency of ligands toward the NR2B NMDA receptors was evaluated by measuring the Ca2t influx evocated by NMDA application (at 100 mM for 30 s) in NR1a/NR2B subunit transfected HEK cells. Radiprodil had potent inhibitory effects (69 nM) towards Ca2+ influx [1]. A low concentration (10?nM) of the GLUN2B receptor antagonist Radiprodil restored LTP in the presence of Aβ1-42, 3NTyr10-Aβ, Aβ1-40, but not AβpE3. Radiprodil (10?nM) reversed the synaptic toxicity of Aβ species but not that of AβpE3 [2].
In vivo	The in vivo analgesic efficiency for 1a in the mouse formalin test was 7.7 mg/kg p.o. (ED50) and a clinical trial is currently conducted with Radiprodil [1].

Synonyms	RGH-896
Molecular Weight	397.4
Formula	C21H20FN3O4
CAS No.	496054-87-6

Storage

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

Solubility Information

DMSO: 220 mg/mL (553.6 mM)

References and Literature

1. Labas R, et al. Synthesis, evaluation and metabolic studies of radiotracers containing a 4-(4-[18F]-fluorobenzyl)piperidin-1-yl moiety for the PET imaging of NR2B NMDA receptors. Eur J Med Chem. 2011 Jun;46(6):2295-309. 2. Rammes G, et al. The NMDA receptor antagonist Radiprodil reverses the synaptotoxic effects of different amyloid-beta (Aβ) species on long-term potentiation (LTP). Neuropharmacology. 2018 Sep 15;140:184-192.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Clinical Compound Library Anti-Parkinson's Disease Compound Library Human Metabolite Library Bioactive Compounds Library Max ReFRAME Related Library Antidepressant Compound Library

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Keywords

Radiprodil 496054-87-6 Membrane transporter/Ion channel Neuroscience NMDAR iGluR Ionotropic glutamate receptors RGH-896 RGH896 inhibit Inhibitor RGH 896 inhibitor

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