UNC9994 hydrochloride
目录号: PL01901 纯度: ≥98%
CAS No. :2108826-33-9
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中文名称
UNC9994 hydrochloride
英文名称
UNC9994 hydrochloride
英文别名
Benzothiazole, 5-​[3-​[4-​(2,​3-​dichlorophenyl)​-​1-​piperidinyl]​propoxy]​-​, hydrochloride (1:1)
Cas No.
2108826-33-9
分子式
C21H23Cl3N2Os
分子量
457.84
包装储存
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
UNC9994 hydrochloride 是一种功能选择性的 β-arrestin 偏向的多巴胺 D2 受体 (D2R) 激动剂,可选择性激活 β- arresttin 招募和信号转导。对 D2R 的 Ki 值为 79 nM。UNC9994 hydrochloride 也是 Gi 调节 cAMP 产生的拮抗剂和 D2R/β-arrestin-2 相互作用的部分激动剂。UNC9994 hydrochloride 具有稳定精神效果。
生物活性
UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D 2 receptor (D 2 R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a K i of 79 nM for D 2 R. UNC9994 hydrochloride is also an antagonist of G i -regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.
性状
Solid
IC50 & Target[1][2]
D3 Receptor 17 nM (Ki) D2 Receptor
体外研究(In Vitro)
UNC9994 hydrochloride induces D2-mediated β-arrestin-2 translocation with an EC50s of 6.1 nM and 448 nM in Tango assay and DiscoveRx assay, respectively.
UNC9994 hydrochloride is an antagonist at 5HT2A and 5HT2B and an agonist at 5HT2C and 5HT1A. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
UNC9994 (2.0 mg/kg; i.p.; once) hydrochloride shows antipsychotic activity that is attenuated in β-arrestin-2 knockout mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: C57BL/6J w
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Allen JA, et al. Discovery of β-arrestin-biased dopamine D2 ligands for probing signal transduction pathways essential for antipsychotic efficacy. Proc Natl Acad Sci U S A. 2011 Nov 8;108(45):18488-93.
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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