1. Membrane Transporter/Ion Channel
    Neuronal Signaling
  2. iGluR
  3. Radiprodil

Radiprodil (Synonyms: RGH-896)

Cat. No.: HY-14777
Handling Instructions

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.

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

Radiprodil Chemical Structure

Radiprodil Chemical Structure

CAS No. : 496054-87-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 190 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Technical Information

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  • References

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[1].

IC50 & Target

NMDA NR2B[1].

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[2].
As for LTP, Radiprodil (10 nM) reverses the synaptic toxicity of 3NTyr-AβAβ1-40 and Aβ1-42 but not that AβpE3-42[2].

In Vivo

Radiprodil could block NMDA currents in Mg2+ insensitive variants, with potencies similar to those obtained without Mg2+[3].
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[3].

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (629.09 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5164 mL 12.5818 mL 25.1636 mL
5 mM 0.5033 mL 2.5164 mL 5.0327 mL
10 mM 0.2516 mL 1.2582 mL 2.5164 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

References
Molecular Weight

397.40

Formula

C₂₁H₂₀FN₃O₄

CAS No.

496054-87-6

SMILES

O=C(NC1=CC=C2NC(OC2=C1)=O)C(N3CCC(CC4=CC=C(F)C=C4)CC3)=O

Storage

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

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Radiprodil
Cat. No.:
HY-14777
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Radiprodil

Cat. No.: HY-14777