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Dizocilpine

Cat. No. M2646
Dizocilpine Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 58  USD58 In stock
50mg USD 212  USD212 In stock
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Quality Control
Biological Activity

Dizocilpine (MK-801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.

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 221.3
Formula C16H15N
CAS Number 77086-21-6
Purity 100.00%
Solubility DMSO 23 mg/mL
Storage at -20°C
References

[1] K Harsha Vardhan Reddy, et al. Convergent Strategy to Dizocilpine MK-801 and Derivatives

[2] Peter Kovacic, et al. Clinical physiology and mechanism of dizocilpine (MK-801): electron transfer, radicals, redox metabolites and bioactivity

[3] T M Tzschentke, et al. Does the noncompetitive NMDA receptor antagonist dizocilpine (MK801) really block behavioural sensitization associated with repeated drug administration?

[4] L J Vanderschuren, et al. Dizocilpine (MK801): use or abuse?

[5] B Geter-Douglass, et al. Dizocilpine-like discriminative stimulus effects of competitive NMDA receptor antagonists in mice

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