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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).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $41 | In Stock | |
2 mg | $59 | In Stock | |
5 mg | $97 | In Stock | |
10 mg | $155 | In Stock | |
25 mg | $253 | In Stock | |
50 mg | $372 | In Stock | |
100 mg | $559 | In Stock | |
1 mL x 10 mM (in DMSO) | $97 | In Stock |
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]. |
Alias | RGH-896 |
Molecular Weight | 397.4 |
Formula | C21H20FN3O4 |
Cas No. | 496054-87-6 |
Smiles | Fc1ccc(CC2CCN(CC2)C(=O)C(=O)Nc2ccc3[nH]c(=O)oc3c2)cc1 |
Relative Density. | 1.394 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 220 mg/mL (553.6 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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