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ML417

  Cat. No.:  DC33653   Featured
Chemical Structure
1386162-69-1
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More than 5000 active chemicals with high quality for research!
Field of application
ML417 is a Highly Selective D3 Dopamine Receptor Agonist. ML417 potently promotes D3R-mediated β-arrestin translocation, G protein activation, and ERK1/2 phosphorylation (pERK) while lacking activity at other dopamine receptors. Screening of ML417 against multiple G protein-coupled receptors revealed exceptional global selectivity. Molecular modeling suggests that 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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1386162-69-1
Chemical Name: 1H-Indol-2-yl[4-[2-(4-methoxyphenoxy)ethyl]-1-piperazinyl]methanone
Synonyms: ML417; ML-417; ML 417;
SMILES: O=C(C(N1)=CC2=C1C=CC=C2)N3CCN(CCOC4=CC=C(OC)C=C4)CC3
Formula: C22H25N3O3
M.Wt: 379.45
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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].
Target: D3 Receptor:38 nM (EC50)
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.
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].
References: [1]. Moritz AE, et al. Discovery, Optimization, and Characterization of ML417: A Novel and Highly Selective D3 Dopamine Receptor Agonist. J Med Chem. 2020;63(10):5526‐5567.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
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