ML417 is a selective and brain penetrantD3dopamine receptor(D3R)agonist, with anEC₅₀of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, andpERKphosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons^[1].

ML417 exhibits a K_ifor the D3R of 1.24 μM. ML417 is a full and potent agonist for multiple signaling pathways associated with D3R activation^[1].
ML417 potently inhibits cAMP accumulation with an EC₅₀of 86 nM and an efficacy identical to that of dopamine. ML417 exhibits submicromolar affinity for only three of the targets, the β1-adrenergic, 5-HT2B serotoninergic, and σ-1 receptors. ML417 stimulates β-arrestin recruitment to the D3R-WT with an EC₅₀of 1.4 nM^[1].
ML417 protects (0.005-5 μM; 24 hours) D3R-expressing dopaminergic neurons from 6-OHDA induced cell death^[1].

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 T_maxof 0.5 hours and C_maxof 6500 ng/ml, and a brain T_maxof 0.25 hours and C_maxof 28000 ng/ml^[1].

379.45

Solid

C₂₂H₂₅N₃O₃

1386162-69-1

Room temperature in continental US; may vary elsewhere.

DMSO : 50 mg/mL(131.77 mM;Need ultrasonic)

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——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
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• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 5 mg/mL (13.18 mM); Clear solution

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  以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。