VU0467485 AZ13713945|cas:1451994-10-7|西域试剂

VU0467485 AZ13713945,99.0%

产品编号：Bellancom-120184| CAS NO：1451994-10-7| 分子式：C₁₇H₁₇FN₄O₂S| 分子量：360.41

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货号	价格	库存与货期
Bellancom-120184	￥2000.00	杭州北京（现货）
Bellancom-120184	￥3200.00	杭州北京（现货）
Bellancom-120184	￥6000.00	杭州北京（现货）
Bellancom-120184	￥9600.00	杭州北京（现货）

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VU0467485 AZ13713945

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。

生物活性

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.

体外研究

体内研究

VU0467485 (1-10 mg/kg; p.o.) has antipsychotic-like activity in an amphetamine-induced hyperlocomotion (AHL) rat model.
VU0467485 (3 mg/kg; p.o.) treatment displays that the C_max, AUC_o-inf and elimination t_1/2 were 1.2 μM, 3.8 μM•h and 4.2 hours, respectively.

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

Animal Model:	Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model)
Dosage:	1, 3, 10 mg/kg
Administration:	Oral administration
Result:	Dose-dependently reverses AHL.

Animal Model:	Male sprague Dawley rats
Dosage:	Oral administration (Pharmacokinetic Analysis)
Administration:	3 mg/kg
Result:	The C_max, AUC_o-inf and elimination t_1/2 were 1.2 μM, 3.8 μM•h and 4.2 hours, respectively.

体内研究

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

Animal Model:	Sprague Dawley rats (amphetamine-induced hyperlocomotion rat model)
Dosage:	1, 3, 10 mg/kg
Administration:	Oral administration
Result:	Dose-dependently reverses AHL.

Animal Model:	Male sprague Dawley rats
Dosage:	Oral administration (Pharmacokinetic Analysis)
Administration:	3 mg/kg
Result:	The C_max, AUC_o-inf and elimination t_1/2 were 1.2 μM, 3.8 μM•h and 4.2 hours, respectively.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (55.49 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7746 mL	13.8731 mL	27.7462 mL
5 mM	0.5549 mL	2.7746 mL	5.5492 mL
10 mM	0.2775 mL	1.3873 mL	2.7746 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式