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PYD-106 

Cat. No. M28598
PYD-106  Structure
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Biological Activity

PYD-106 is a stereoselective pyrrolidinone (PYD) positive allosteric modulator for GluN2C-containing NMDA receptors. PYD-106 increases opening frequency and open time of single channel currents activated by maximally effective concentrations of agonist but only has modest effects on glutamate and glycine EC50. PYD-106 selectively enhances the responses of diheteromeric GluN1/GluN2C receptors but not triheteromeric GluN1/GluN2A/GluN2C receptors.

Chemical Information
Molecular Weight 432.47
Formula C25H24N2O5
CAS Number 1560894-05-4
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Elena Bechthold, et al. Biol Chem. In vitro ADME characterization of a very potent 3-acylamino-2-aminopropionic acid-derived GluN2C-NMDA receptor agonist and its ester prodrugs

[2] David H Hackos, et al. Neuropharmacology. Diverse modes of NMDA receptor positive allosteric modulation: Mechanisms and consequences

[3] Thomas M Kaiser, et al. Mol Pharmacol. The Bioactive Protein-Ligand Conformation of GluN2C-Selective Positive Allosteric Modulators Bound to the NMDA Receptor

[4] Tsung-Han Chou, et al. Mol Cell. Structural insights into assembly and function of GluN1-2C, GluN1-2A-2C, and GluN1-2D NMDARs

[5] Alpa Khatri, et al. Mol Pharmacol. Structural determinants and mechanism of action of a GluN2C-selective NMDA receptor positive allosteric modulator

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Keywords: PYD-106  supplier, GluR, inhibitors, activators


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