1. GPCR/G Protein
    Neuronal Signaling
  2. Dopamine Receptor
  3. ML417

ML417 

Cat. No.: HY-136390 Purity: 99.65%
Handling Instructions

ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons.

For research use only. We do not sell to patients.

ML417 Chemical Structure

ML417 Chemical Structure

CAS No. : 1386162-69-1

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 500 In-stock
Estimated Time of Arrival: December 31
100 mg USD 800 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

ML417 is a selective and brain penetrant D3 dopamine receptor (D3R) agonist, with an EC50 of 38 nM. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein mediated signaling, and pERK phosphorylation with minimal effects on other GPCR-mediated signaling. ML417 exhibits neuroprotection against toxin-induced neurodegeneration of dopaminergic neurons[1].

IC50 & TargetHY-P7488

D3 Receptor

38 nM (EC50)

In Vitro

ML417 exhibits a Ki for 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 EC50 of 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 EC50 of 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

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[1].

Animal Model: 6-8 week old male C57BL/6 mice[1]
Dosage: 20 mg/kg
Administration: I.p. (Pharmacokinetic Analysis)
Result: Brain penetrant and exhibits a plasma half-life of 3.44 hours and a brain half-life of 4.23 hours. Displayed 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.
Molecular Weight

379.45

Formula

C₂₂H₂₅N₃O₃

CAS No.

1386162-69-1

SMILES

O=C(C(N1)=CC2=C1C=CC=C2)N3CCN(CCOC4=CC=C(OC)C=C4)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6354 mL 13.1770 mL 26.3539 mL
5 mM 0.5271 mL 2.6354 mL 5.2708 mL
10 mM 0.2635 mL 1.3177 mL 2.6354 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

ML417ML 417ML-417Dopamine Receptorβ-arrestintranslocationphosphorylationneuroprotectiondopaminergicneuronsInhibitorinhibitorinhibit

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ML417
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HY-136390
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