PQCA
目录号: PL06852 纯度: ≥99%
CAS No. :1144504-35-7
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中文名称
PQCA
中文别名
1-((4-氰基-4-(吡啶-2-基)哌啶-1-基)甲基)-4-氧代-4H-喹嗪-3-羧酸
英文名称
PQCA
英文别名
1-((4-cyano-4-(pyridin-2-yl)piperidin-1-yl)methyl)-4-oxo-4H-quinolizine-3-carboxylic acid;PQCA;BDBM50348232;1-[(4-Cyano-4-pyridin-2-ylpiperidin-1-yl)methyl]-4-oxoquinolizine-3-carboxylic acid
Cas No.
1144504-35-7
分子式
C22H20N4O3
分子量
388.42
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PQCA 是一种高度选择性且有效的毒蕈碱 M1 受体阳性变构调节剂。PQCA 在恒河猴和人 M1 受体上的 EC50 值分别为 49 nM 和 135 nM,并对其他毒蕈碱受体无活性。PQCA 具有减少与阿尔茨海默氏病相关的认知缺陷的潜力。
生物活性
PQCA is a highly selective and potent muscarinic M1 receptor positive allosteric modulator. PQCA has an EC 50 value of 49 nM and 135 nM on rhesus and human M1 receptor, respectively. PQCA is inactive for other muscarinic receptors. PQCA has potential to reduce the cognitive deficits associated with Alzheimers disease.
性状
Solid
IC50 & Target[1][2]
EC50: 49 nM (Rhesus M1 receptor) and 135 nM (Human M1 receptor)
体内研究(In Vivo)
PQCA (3-30 mg/kg; oral administration; single- or pair-housed male rhesus monkeys) treatment attenuates the scopolamine deficits in PAL and CPT tasks. Blockade of muscarinic signaling by scopolamine produces significant impairments in both tasks. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Lange HS, et al. The M1 Muscarinic Positive Allosteric Modulator PQCA Improves Performance on Translatable Tests of Memory and Attention in Rhesus Monkeys. J Pharmacol Exp Ther. 2015 Dec;355(3):442-50.
[2]. Uslaner JM, et al. The muscarinic M1 receptor positive allosteric modulator PQCA improves cognitive measures in rat, cynomolgus macaque, and rhesus macaque. Psychopharmacology (Berl). 2013 Jan;225(1):21-30.
溶解度数据
In Vitro: DMSO : 10 mg/mL (25.75 mM; ultrasonic and warming and heat to 80°C)配制储备液
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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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