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DQP-1105 

Cat. No. M30021
DQP-1105  Structure
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Biological Activity

DQP-1105 is a potent noncompetitive NMDA receptor antagonist. DQP-1105 inhibits GluN2C- and GluN2D-containing receptors (IC50=7.0 and 2.7 μM, respectively). The IC50 values are at least 50-fold lower than those for recombinant GluN2A-, GluN2B-, GluA1-, or GluK2-containing receptors.

Chemical Information
Molecular Weight 558.42
Formula C29H24BrN3O4
CAS Number 380560-89-4
Form Solid
Solubility (25°C) DMSO 10 mg/mL (ultrasonic and warming and heat to 60°C)
Storage 4°C, sealed
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] Huiru Xue, et al. Front Immunol. The circadian rhythms regulated by Cx43-signaling in the pathogenesis of Neuromyelitis Optica

[2] Emese Pálfi, et al. J Sleep Res. Acute blockade of NR2C/D subunit-containing N-methyl-D-aspartate receptors modifies sleep and neural oscillations in mice

[3] Paul G Morris, et al. Front Cell Neurosci. Altered Synaptic and Extrasynaptic NMDA Receptor Properties in Substantia Nigra Dopaminergic Neurons From Mice Lacking the GluN2D Subunit

[4] Sharon A Swanger, et al. J Neurosci. NMDA Receptors Containing the GluN2D Subunit Control Neuronal Function in the Subthalamic Nucleus

[5] Timothy M Acker, et al. Mol Pharmacol. Mechanism for noncompetitive inhibition by novel GluN2C/D N-methyl-D-aspartate receptor subunit-selective modulators

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