SK609 hydrochloride 

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].

In a Competitive inhibition affinity assay by SK609 to D3R, SK609 exhibits an EC₅₀ value of 1109 ± 273 nM at D3R^[1].
SK609 hydrochloride activates Gi/o proteins and downstream ERK1/2 signaling but have no effects on D2R/ERK1/2. SK609 exhibits EC₅₀ values of 1.1 ± 0.2 μM, 50.2 ± 5.9 nM, and 14.4 ± 2.7 μM for [³⁵S]GTPγS binding, ERK1/2 phosphorylation, and β-Arrestin recruitment respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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 C_max values of 13.7, 69.3 and 218 ng/ml respectively, occurring at (T_max) 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

220.14

C₁₀H₁₅Cl₂N

1092797-77-7

CC(CCC1=CC=CC=C1Cl)N.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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  [Content Brief]

  [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.  [Content Brief]