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PD-168077 maleate

Cat. No. M9482
PD-168077 maleate Structure
Size Price Availability Quantity
5mg USD 100  USD100 In stock
10mg USD 150  USD150 In stock
50mg USD 520  USD520 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PD-168077 maleate is a potent D4 dopamine receptor agonist (Ki = 8.7 nM), with > 400-fold and > 300-fold selectivity over D2 / D3 subtypes, respectively. 

In vivo, PD-168077 (0.2-25.0 mg/kg) dose-dependently induces locomotion, which takes an unusual and characteristic ”shuffling” form with uncoordinated movements together with yawning, and episodes of myoclonic jerking; grooming, and rearing are reduced.

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 450.49
Formula C24H26N4O5
CAS Number 630117-19-0
Purity >98%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

[1] Navakkode S, et al. Sci Rep. Bidirectional modulation of hippocampal synaptic plasticity by Dopaminergic D4-receptors in the CA1 area of hippocampus.

[2] Gu Z, et al. Mol Pharmacol. Activation of dopamine D4 receptors induces synaptic translocation of Ca2+/calmodulin-dependent protein kinase II in cultured prefrontal cortical neurons.

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