SK609 hydrochloride

CAS: 1092797-77-7 F: C10H15Cl2N W: 220.14

SK609 hydrochloride is a dopamine D3 receptor (D3R) selective agonist with an EC50 of 1109 nM. SK609 hydrochloride has t

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Bioactivity	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].
Invitro	在 SK609 对 D3R 的竞争性抑制亲和实验中，SK609 对 D3R 处的 EC50 值为 1109±273 nM[1]。 SK609 激活 Gi/o 蛋白和下游 ERK1/2 信号，但对 D2R/ERK1/2 无影响。SK609 对 [35S]GTPγS 结合、ERK1/2 磷酸化和 β-捕集蛋白的 EC50 值分别为 1.1±0.2 μM、50.2±5.9 nM 和 14.4±2.7 μM [1]。
In Vivo	SK609 在大鼠中的安全毒理学研究表明，SK609 的最大耐受剂量为30mg/kg，本研究中使用的所有剂量均在SK609[1]。在食蟹猴 PK 研究中，口服 SK609 (P.O.; 0.5、2和4 mg/kg) 与给药后 4.1、6.4 和 5.0 小时 (Tmax) 的平均Cmax 值分别为 13.7、69.3 和 218 ng/mL，相应的 AUC (0-t) 值分别为 171、904 和 2938 h.ng/mL[3]。静脉给药 (2mg /kg) 后，SK609在血浆中的平均终末半衰期为7.9 h。SK609 (i.p.; 2、4、6、8、10、20 mg/kg) 在大鼠的帕金森模型中，可显著改善偏瘫大鼠双侧不对称的功能，并使其恢复正常[3]。
Name	SK609 hydrochloride
CAS	1092797-77-7
Formula	C10H15Cl2N
Molar Mass	220.14
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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 [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.