| Identification | Back Directory | [Name]
SK 609 | [CAS]
1092797-77-7 | [Synonyms]
SK 609
SK609 HCl
SK609 hydrochloride
SK-609 hydrochloride
SK 609 hydrochloride
SK609 hydrochloride (ES609)
SK609 hydrochloride >=98% (HPLC) | [Molecular Formula]
C10H15Cl2N | [MOL File]
1092797-77-7.mol | [Molecular Weight]
220.14 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [color ]
Off-white to light brown | [Water Solubility ]
H2O: 2mg/mL, clear |
| Hazard Information | Back Directory | [Uses]
SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC50 of 1109 nM. SK609 hydrochloride has the potential for parkinson research[1]. | [Biological Activity]
SK609 (ES609) is a Dopamine D3 receptor (D3R) selective agonist with a bias towards the G-protein-dependent pathway rather than recruiting β-arrestin-2 and an EC50 value of 113.9 nM for activation of ERK1/2 phosphorylation. SK609 has been shown to reverse akinesia and reduce L-dopa-induced dyskinesia in a hemiparkinsonian r at model of Parkinsonμs desease. It does not induce desensitization of D3R. | [in vivo]
Safety toxicology studies of SK609 in rats have shown the maximum tolerated dose of SK609 is 30mg/kg and all the doses used in this study are well within the no-observed-adverse-effect level of SK609[1].
SK609 shows the maximum tolerated dose of SK609 is 30mg/kg in safety toxicology study within the no-observed-adverse-effect level of SK609[2].
In the cynomolgus macaques PK study, oral administration of SK609 (0.5, 2 and 4 mg/kg) is associated with mean Cmax values of 13.7, 69.3 and 218 ng/ml respectively, occurring at (Tmax) 4.1, 6.4 and 5.0 hours following administration and with corresponding AUC(0-t) values of 171, 904 and 2938 h.ng/ml respectively[3].Following intravenous administration (2 mg/kg), SK609 had a mean terminal half-life of 7.9 h in plasma.?SK609 (i.p.; 2, 4, 6, 8, 10, 20 mg/kg) significantly improves the performance of the impaired paw and also normalized the bilateral asymmetry associated with the hemiparkinson rat[3]. | [IC 50]
Dopamine D3 receptor: 1109 nM (EC50) | [storage]
Store at -20°C | [References]
[1] Wei Xu, et al. Functional Characterization of a Novel Series of Biased Signaling Dopamine D3 Receptor Agonists. ACS Chem Neurosci. 2017 Mar 15;8(3):486-500. DOI:10.1021/acschemneuro.6b00221
[2] Jay S Schneider, et al. A novel dopamine D3R agonist SK609 with norepinephrine transporter inhibition promotes improvement in cognitive task performance in rodent and non-human primate models of Parkinson's disease. Exp Neurol. 2021 Jan;335:113514 DOI:10.1016/j.expneurol.2020.113514
[3] Sherise L Simms, et al. In vivo characterization of a novel dopamine D3 receptor agonist to treat motor symptoms of Parkinson's disease . Neuropharmacology. 2016 Jan;100:106-15. DOI:10.1016/j.neuropharm.2015.04.004 |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
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21-20338288 |
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www.sigmaaldrich.cn |
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