UNC9994 hydrochloride,98.83%

产品编号:Bellancom-111385| CAS NO:2108826-33-9| 分子式:C21H23Cl3N2OS| 分子量:457.84

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-111385
3500.00 杭州 北京(现货)
Bellancom-111385
7000.00 杭州 北京(现货)
Bellancom-111385
11000.00 杭州 北京(现货)

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UNC9994 hydrochloride

产品介绍 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 D2RKi 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 D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

UNC9994 (2.0 mg/kg; i.p.; once) hydrochloride shows antipsychotic activity that is attenuated in β-arrestin-2 knockout mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J wild-type and β-arrestin-2 knockout mice
Dosage: 2.0 mg/kg, followed 30 min later with 6 mg/kg phencyclidine (PCP, i.p.)
Administration: IP, once
Result: Markedly inhibited PCP-induced hyperlocomotion in wild-type mice and the activity was completely abolished in β-arrestin-2 knockout mice.
体内研究

UNC9994 (2.0 mg/kg; i.p.; once) hydrochloride shows antipsychotic activity that is attenuated in β-arrestin-2 knockout mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J wild-type and β-arrestin-2 knockout mice
Dosage: 2.0 mg/kg, followed 30 min later with 6 mg/kg phencyclidine (PCP, i.p.)
Administration: IP, once
Result: Markedly inhibited PCP-induced hyperlocomotion in wild-type mice and the activity was completely abolished in β-arrestin-2 knockout mice.
性状Solid
溶解性数据
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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