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Radiprodil (RGH-896)

Cat. No. M10606
Radiprodil (RGH-896) Structure
Synonym:

RGH-896

Size Price Availability Quantity
5mg USD 120  USD120 In stock
25mg USD 420  USD420 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

Radiprodil (also known as RGH-896) is an orally active and selective NMDA receptors antagonist which was evaluated as potential treatment of neuropathic pain associated with diabetic peripheral neuropathy (DPNP). Radiprodil could block NMDA currents in Mg2+ insensitive variants, with potencies similar to those obtained without Mg2+.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 397.40
Formula C21H20FN3O4
CAS Number 496054-87-6
Purity >98.5%
Solubility DMSO ≥ 80 mg/mL
Storage at -20°C
References

[1] Gerhard Rammes, et al. Neuropharmacology. The NMDA receptor antagonist Radiprodil reverses the synaptotoxic effects of different amyloid-beta (Aβ) species on long-term potentiation (LTP)

[2] Brice Mullier, et al. Neuropharmacology. GRIN2B gain of function mutations are sensitive to radiprodil, a negative allosteric modulator of GluN2B-containing NMDA receptors

[3] Alda Fernandes, et al. Eur J Pharmacol. Inhibition of in vivo [(3)H]MK-801 binding by NMDA receptor open channel blockers and GluN2B antagonists in rats and mice

[4] Laetitia Mony, et al. Br J Pharmacol. Allosteric modulators of NR2B-containing NMDA receptors: molecular mechanisms and therapeutic potential

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Keywords: Radiprodil (RGH-896), RGH-896 supplier, NMDA, inhibitors

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