ML417 manufacturers
- ML417
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- $34.00 / 2mg
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2024-11-17
- CAS:1386162-69-1
- Min. Order:
- Purity: 99.42%
- Supply Ability: 10g
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| Product Name: | ML417 | | Synonyms: | ML417;Methanone, 1H-indol-2-yl[4-[2-(4-methoxyphenoxy)ethyl]-1-piperazinyl]-;neuroprotection,dopaminergic,β-arrestin,ML417,ML-417,translocation,phosphorylation,neurons,ML 417,Inhibitor,Dopamine Receptor,inhibit;(1H-indol-2-yl)(4-(2-(4-methoxyphenoxy)ethyl)piperazin-1-yl)methanone;2-{4-[2-(4-methoxyphenoxy)ethyl]piperazine-1-carbonyl}-1H-indole;ML417, 10 mM in DMSO | | CAS: | 1386162-69-1 | | MF: | C22H25N3O3 | | MW: | 379.45 | | EINECS: | | | Product Categories: | | | Mol File: | 1386162-69-1.mol |  |
| | ML417 Chemical Properties |
| Boiling point | 613.3±55.0 °C(Predicted) | | density | 1.231±0.06 g/cm3(Predicted) | | storage temp. | 2-8°C | | solubility | DMSO: 2mg/mL, clear | | form | Solid | | pka | 16.11±0.30(Predicted) | | color | Off-white to light yellow |
| | ML417 Usage And Synthesis |
| Uses | 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]. | | Biological Activity | ML417 is a blood-brain barrier permeable, potent and highly selective agonist of D3 dopamine receptor (D3R) with very limited cross-reactivity at other GPCRs. ML417 potently induces G-protein activation, D3R-mediated b-arrestin translocation and pERK phosphorylation. It does not activate other dopamine receptors. ML417 protect D3R-expressing dopaminergic neurons from 6-OHDA induced cell death. | | 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.
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| | IC 50 | D3 Receptor: 38 nM (EC50) | | 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. DOI:10.1021/acs.jmedchem.0c00424 |
| | ML417 Preparation Products And Raw materials |
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