VU0467485

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VU0467485

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1451994-10-7

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
50mg	电议
100mg	电议

产品介绍

VU0467485 (AZ13713945) 是一种有效的、选择性的、口服生物可利用的毒蕈碱乙酰胆碱受体 4 (M4) 正变构调节剂 (PAM)。VU0467485 (AZ13713945) 增强了 ACh 在 M4 的活性，在大鼠和人 M4 受体上的 EC50 分别为 26.6 nM 和 78.8 nM。VU0467485 (AZ13713945) 显示 M4 对人和大鼠 M1/2/3/5 的选择性。VU0467485 (AZ13713945) 显示中度至高度中枢神经系统渗透，并具有抗精神病样活性。

Cas No.	1451994-10-7
别名	AZ13713945
Canonical SMILES	O=C(C1=C(N)C2=C(C)C(C)=NN=C2S1)NCC3=CC=C(OC)C(F)=C3
分子式	C₁₇H₁₇FN₄O₂S
分子量	360.41
溶解度	Soluble in DMSO
储存条件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request
产品描述	VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity[1]. VU0467485 (1-10 mg/kg; p.o.) has antipsychotic-like activity in an amphetamine-induced hyperlocomotion (AHL) rat model[1].VU0467485 (3 mg/kg; p.o.) treatment displays that the Cmax, AUCo-inf and elimination t1/2 were 1.2 μM, 3.8 μM•h and 4.2 hours, respectively[1]. Animal Model: Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model) [1] [1]. Wood MR, et al. Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia. ACS Med Chem Lett. 2016 Dec 16;8(2):233-238.