Description
Radiprodil (RGH-896) is an orally active and selective NMDA NR2B antagonist. A potential therapeutic agent in treatment of neuropathic pain and possibly other chronic pain conditions.
Product information
CAS Number: 496054-87-6
Molecular Weight: 397.40
Formula: C21H20FN3O4
Chemical Name: 2-{4-[(4-fluorophenyl)methyl]piperidin-1-yl}-2-oxo-N-(2-oxo-2,3-dihydro-1,3-benzoxazol-6-yl)acetamide
Smiles: O=C1NC2=CC=C(C=C2O1)NC(=O)C(=O)N1CCC(CC2C=CC(F)=CC=2)CC1
InChiKey: GKGRZLGAQZPEHO-UHFFFAOYSA-N
InChi: InChI=1S/C21H20FN3O4/c22-15-3-1-13(2-4-15)11-14-7-9-25(10-8-14)20(27)19(26)23-16-5-6-17-18(12-16)29-21(28)24-17/h1-6,12,14H,7-11H2,(H,23,26)(H,24,28)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 250 mg/mL (629.09 mM; Need ultrasonic).
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:
Preincubation with Radiprodil (10 nM) restores long-term potentiation (LTP) in the presence of Aβ1-42, 3NTyr10-Aβ and Aβ1-40, but not AβpE3. As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AβAβ1-40 and Aβ1-42 but not that AβpE3-42.
In Vivo:
Radiprodil could block NMDA currents in Mg2+ insensitive variants, with potencies similar to those obtained without Mg2+. Radiprodil's potency is higher at pH 7.0 than at pH 7.6, suggesting that radiprodil may retain its ability to block glutamate-induced NMDA currents even under acidic conditions that manifest under long term seizures.
Products are for research use only. Not for human use.
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