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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 & Documentation
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+.

Chemical Information
Molecular Weight 397.40
Formula C21H20FN3O4
CAS Number 496054-87-6
Solubility (25°C) DMSO ≥ 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

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, activators


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