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SK609 hydrochloride
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SK609 hydrochloride
CAS No. : 1092797-77-7
MCE 站:SK609 hydrochloride
产品活性:SK609 hydrochloride 是一种多巴胺 D3 受体 (D3R) 选择性激动剂,EC50 为 1109 nM。SK609 hydrochloride 可用于帕金森病的研究。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Dopamine Receptor
In Vitro: In a Competitive inhibition affinity assay by SK609 to D3R, SK609 exhibits an EC50 value of 1109 ± 273 nM at D3R.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.
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.SK609 shows the maximum tolerated dose of SK609 is 30mg/kg in safety toxicology study within the no-observed-adverse-effect level of SK609.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.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.
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