VU0483605
目录号 : GC11667
A selective mGlu1 PAM
Cas No.:1623101-11-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1 [1].
The metabotropic glutamate receptors (mGluRs), members of G-protein-coupled receptors, have been involved in a variety of functions in the central and peripheral nervous systems, such as learning, memory, anxiety, and the perception of pain. The mGluRs exist in pre- and postsynaptic neurons in synapses of the hippocampus, cerebellum, the cerebral cortex, as well as other parts of the brain and in peripheral tissues. Mice deficient in mGluR1 showed severe motor coordination and spatial learning deficient [2].
VU0483605 is a selective positive allosteric modulator (PAM) of mGluR1. VU0483605 displayed EC50 values of 0.39 and 0.36 μM at human and rat mGluR1 receptors, respectively. VU0483605 showed no activity against mGlu4 PAM with the EC50 of >10 μM. VU0483605 potentiated the response to glutamate in cells stably expressing mGlu1 and partially restored the reduction in glutamate-mediated calcium signaling in a mutant cell model of schizophrenia [1].
References:
[1] Cho H P, Garcia-Barrantes P M, Brogan J T, et al. Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics[J]. ACS chemical biology, 2014, 9(10): 2334-2346.
[2] Conquet F, Bashir Z I, Davies C H, et al. Motor deficit and impairment of synaptic plasticity in mice lacking mGluR1[J]. Nature, 1994, 372(6503): 237.
| Cas No. | 1623101-11-0 | SDF | |
| 化学名 | 3-chloro-N-[3-chloro-4-(4-chloro-1,3-dihydro-1,3-dioxo-2H-isoindol-2-yl)phenyl]-2-pyridinecarboxamide | ||
| Canonical SMILES | O=C1N(C2=CC=C(NC(C3=C(Cl)C=CC=N3)=O)C=C2Cl)C(C4=CC=CC(Cl)=C41)=O | ||
| 分子式 | C20H10Cl3N3O3 | 分子量 | 446.7 |
| 溶解度 | ≤20mg/ml in DMSO;20mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2386 mL | 11.1932 mL | 22.3864 mL |
| 5 mM | 0.4477 mL | 2.2386 mL | 4.4773 mL |
| 10 mM | 0.2239 mL | 1.1193 mL | 2.2386 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。