VU 0364439
(Synonyms: N-[3-氯-4-[[(2-氯苯基)氨基]磺酰基]苯基]-2-吡啶甲酰胺) 目录号 : GC16150
A positive allosteric modulator of mGluR4
Cas No.:1246086-78-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
VU 0364439 is a positive allosteric modulator (PAM) of mGlu4 with an EC50 value of 19.8 nM [1] [2] [3].
MGlu4 belongs to metabotropic glutamate receptor (mGluR) group III which contains mGlu4, mGlu6, mGlu7 and mGlu8. MGluRs belong to Class C of G-protein-coupled receptor (GPCR) superfamily. GPCRs modulate postsynaptic effects or the release of glutamate [2].
VU 0364439 exhibited excellent in vitro maximal response and potency relative to another PAM, (−)-PHCCC (a partially selective mGlu4 potentiator, its chemical structure could be found in reference 4). Starting at 30µM, using a 1:3 serial dilutions, VU 0364439 was tested in triplicate. The entire test was performed on one day. Finally, the % (−)-PHCCC value of VU 0364439 was 102.3. The value of % (−)-PHCCC was computed through dividing the maximal response elicited by VU 0364439 by the response of the control PAM, (−)-PHCCC, on the same day. It was also found that the EC50 value of VU 0364439 was 19.8 nM at human mGlu4 [4].
VU 0364439 possessed less than ideal pharmacokinetic properties. The properties of VU 0364439 prevents VU 0364439 itself from being used as an in vivo tool, but VU 0364439 might inform the mGlu4 community with more in vitro tool compounds [4].
References:
[1]. Lucyna Pomierny-Chamioło, Kinga Rup, Bartosz Pomierny, et al. Metabotropic glutamatergic receptors and their ligands in drug addiction. Pharmacology & Therapeutics, 2014, 142:281-305.
[2]. Albert J. Robichaud, Darren W. Engers, Craig W. Lindsley, et al. Recent Progress on the Identification of Metabotropic Glutamate 4 Receptor Ligands and Their Potential Utility as CNS Therapeutics. ACS Chemical Neuroscience, 2011, 2:433-449.
[3]. Colleen M. Niswender, Kari A. Johnson, C. David Weaver, et al. Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4. Mol. Pharmacol., 2008, 74(5):1345-1358.
[4]. Darren W. Engers, Patrick R. Gentry, Richard Williams, et al. Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorg. Med. Chem. Lett., 2010, 20:5175-5178.
| Cas No. | 1246086-78-1 | SDF | |
| 别名 | N-[3-氯-4-[[(2-氯苯基)氨基]磺酰基]苯基]-2-吡啶甲酰胺 | ||
| 化学名 | N-[3-chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl]pyridine-2-carboxamide | ||
| Canonical SMILES | C1=CC=C(C(=C1)NS(=O)(=O)C2=C(C=C(C=C2)NC(=O)C3=CC=CC=N3)Cl)Cl | ||
| 分子式 | C18H13Cl2N3O3S | 分子量 | 422.29 |
| 溶解度 | ≥ 21.1mg/mL in DMSO | 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 | 2.368 mL | 11.8402 mL | 23.6804 mL |
| 5 mM | 0.4736 mL | 2.368 mL | 4.7361 mL |
| 10 mM | 0.2368 mL | 1.184 mL | 2.368 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。