VU0364770 hydrochloride
目录号 : GC38597
An mGluR4 and mGluR6 positive allosteric modulator and mGluR5 antagonist
Cas No.:1414842-70-8
Sample solution is provided at 25 µL, 10mM.
VU0364770 is a positive allosteric modulator of metabotropic glutamate receptor 4 (mGluR4; EC50 = 1.1 ?M in a calcium mobilization assay).1 It is also a positive allosteric modulator of mGluR6 (EC50 = 6.8 ?M) and an antagonist of mGluR5 (IC50 = 17.9 ?M). VU0364770 binds to monoamine oxidase A (MAO-A) and MAO-B (Kis = 8.5 and 7.2 ?M, respectively), as well as the human norepinephrine transporter in a panel of 68 receptors, ion channels, and transporters at 10 ?M. It decreases haloperidol-induced catalepsy and reduces increases in the number of premature reactions in response to a light cue, indicating improved attentional control, in a 6-hydroxydopamine rat model of Parkinson’s disease when administered at a dose of 56.6 mg/kg.
1.Jones, C.K., Bubser, M., Thompson, A.D., et al.The metabotropic glutamate receptor 4-positive allosteric modulator VU0364770 produces efficacy alone and in combination with ?-DOPA or an adenosine 2A antagonist in preclinical rodent models of Parkinson's diseaseJ. Pharmacol. Exp. Ther.340(2)404-421(2012)
Cas No. | 1414842-70-8 | SDF | |
Canonical SMILES | O=C(C1=NC=CC=C1)NC2=CC=CC(Cl)=C2.[H]Cl | ||
分子式 | C12H10Cl2N2O | 分子量 | 269.13 |
溶解度 | DMSO: 100 mg/mL (371.57 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
1 mM | 3.7157 mL | 18.5784 mL | 37.1568 mL |
5 mM | 0.7431 mL | 3.7157 mL | 7.4314 mL |
10 mM | 0.3716 mL | 1.8578 mL | 3.7157 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >99.50%
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