2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. VU6025733

VU6025733 (AG06827) 是一种高选择性、口服有效且能透过血脑屏障的毒蕈碱型乙酰胆碱受体亚型 M4 (M4 mAChR) 正向变构调节剂。VU6025733 可增强乙酰胆碱诱导的受体活化，对 hM4 的 EC50 为 23 nM，对 rM4 的 EC50 为 55 nM。VU6025733 对其他毒蕈碱型乙酰胆碱受体亚型具有高度选择性，并能剂量依赖性地降低苯丙胺诱导的大鼠活动过度。 VU6025733 适用于精神分裂症、帕金森病和阿尔茨海默病的研究。

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VU6025733

VU6025733 Chemical Structure

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VU6025733 相关抗体

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VU6025733 (AG06827) is a highly selective, orally active and blood-brain barrier-penetrant positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4 (M4 mAChR). VU6025733 exerts a potentiating effect on acetylcholine-induced receptor activation with an EC50 of 23 nM for hM4 and 55 nM for rM4. VU6025733 shows high selectivity over other muscarinic acetylcholine receptor subtypes, dose-dependently reduces amphetamine-induced hyperlocomotion in rats. VU6025733 is applicable to the research of schizophrenia, Parkinson's disease, and Alzheimer's disease[1].

体外研究
(In Vitro)

VU6025733 可强效增强人源 M4/Gqi5-CHO 细胞的活性 (EC50 = 33 nM) 和大鼠源 M4/Gqi5-CHO 细胞的活性 (EC50 = 62 nM)，但在表达人源或大鼠源 M1、M2、M3 或 M5 毒蕈碱受体的 CHO 细胞中无活性[1]。
VU6025733 以 4.6 μM 的 IC50 抑制 hERG 通道[1]。
VU6025733 可在 HepaRG 3D 球体中诱导细胞毒性作用，包括降低谷胱甘肽含量和细胞内 ATP 水平，其 MEC 值分别为 9.7 μM 和 4.2 μM[1]。
VU6025733 可降低 HepG2 细胞的耗氧率 (MEC = 2.0 μM) 并提高其胞外酸化率 (MEC = 7.1 μM)，表明其可抑制电子传递链[1]。
VU6025733 具有较高的脑渗透潜力，且无 P-糖蛋白外排作用；正如在 MDCKII-MDR1 细胞中测得的外排比 0.80 以及 Papp (A-B) 为 12.7 × 10-6 cm/s 所显示的那样[1]。
VU6025733 对 CYP1A2、CYP2C9 和 CYP3A4 的抑制作用极弱 (IC50 ≥ 19.3 μM)，对 CYP2D6 具有中等抑制作用 (IC50 = 8.4 μM)[1]。

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

VU6025733 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 MRT CLplasma Vss Plasma Concentration CLunbound Brain Concentration Brain distribution Tmax Cmax AUC0-∞ Bioavailability
Rat[1] 1 mg/kg i.v. 5.67 h 3.83 h 5.26 mL/min/kg 1.21 L/kg / / / / / / / /
Rat[1] 3 mg/kg p.o. / / / / / / / / 0.75 h 1783 ng/mL 6753 ng·h/mL 74.1 %
Rat[1] 10 mg/kg p.o. / / / / 3974 ng/mL 39.7 ng/mL 1086 ng/g 17.4 ng/g / / / /
Rat[1] 15 mg/kg p.o. / / / / 6463 ng/mL 64.6 ng/mL 1587 ng/g 25.4 ng/g / / / /
Rat[1] 30 mg/kg p.o. / / / / 11477 ng/mL 115 ng/mL 3157 ng/g 50.5 ng/g / / / /
体内研究
(In Vivo)

VU6025733 (10-30 mg/kg; p.o.) 可在雄性 Sprague-Dawley 大鼠中对精神活性物质诱导的过度活动产生显著的、剂量依赖性的阻断作用，其最低有效剂量为 10 mg/kg，在最高测试剂量下逆转率可达 39.7%[1]。

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

Animal Model: Sprague-Dawley (male)[1]
Dosage: 10 mg/kg; 15 mg/kg; 30 mg/kg
Administration: p.o.; single administration
Result: Produced a 25.6% reversal of induced hyperlocomotion, with a mean unbound brain concentration of 17.4 ng/g.
Produced a 34.0% reversal of induced hyperlocomotion, with a mean unbound brain concentration of 25.4 ng/g.
Produced a 39.7% reversal of induced hyperlocomotion, with a mean unbound brain concentration of 50.5 ng/g.
Significantly reduced total ambulation.
分子量

386.46

Formula

C20H18D5N5O3
非标记 CAS
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

VU6025733 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU6025733AG06827VU 6025733VU-6025733AG 06827AG-06827mAChRMuscarinic acetylcholine receptorM4 muscarinic acetylcholine receptor positive allosteric modulatororally activeblood-brain barrier penetrantpotentiate acetylcholine-mediated M4 mAChR activationhM4/Gqi5-CHO cellsMDCKII-MDR1 transfected cellsHepaRG 3D spheroidsHepG2 cellsrat amphetamine-induced hyperlocomotion modelSD ratschizophreniaParkinson's diseaseAlzheimer's diseaseInhibitorinhibitorinhibit

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产品名称：
VU6025733
目录号：
HY-181559S
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