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ML417

Cat. No. M10494
ML417 Structure
Synonym:

ML-417

Size Price Availability Quantity
10mg USD 148  USD148 In stock
50mg USD 440  USD440 In stock
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Quality Control & Documentation
Biological Activity

ML417 is a highly selective and brain penetrant D3 dopamine receptor (D3R) agonist, with EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein activation, and ERK1/2 phosphorylation (pERK) while lacking activity at other dopamine receptors. ML417 interacts with the D3R in a unique manner, possibly explaining its remarkable selectivity. ML417 was also found to protect against neurodegeneration of dopaminergic neurons derived from iPSCs.

In vivo pharmacokinetics experiments in mice (using 20 mg/kg; i.p.) reveals that ML417 is brain penetrant and exhibits a plasma half-life of 3.44 hours and a brain half-life of 4.23 hours. ML417 displays a plasma Tmax of 0.5 hours and Cmax of 6500 ng/ml, and a brain Tmax of 0.25 hours and Cmax of 28000 ng/ml.

Chemical Information
Molecular Weight 379.45
Formula C22H25N3O3
CAS Number 1386162-69-1
Solubility (25°C) DMSO 45 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] Amy E Moritz, et al. J Med Chem. Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D 3 Dopamine Receptor Agonist

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