CAS NO: | 1246086-78-1 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
25mg | 电议 |
100mg | 电议 |
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 422.29 |
Cas No. | 1246086-78-1 |
Formula | C18H13Cl2N3O3S |
Solubility | ≥21.11 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
VU 0364439 是mGluR4的正向变构调节剂(PAM),EC50值为19.8 nM[1][2][3]。
MGlu4属于代谢型谷氨酸受体(mGluR)家族III,该家族包括mGlu4、mGlu6、mGlu7和mGlu8。MGluR属于C类G蛋白偶联受体(GPCR)超家族。GPCRs调控突触后效应或谷氨酸的释放[2]。
在体外,相比另一个PAM,()-PHCCC(一种部分选择性的mGlu4增效剂,其分子结构参见参考文献4),VU 0364439表现出优异的最大反应和效力。VU 0364439从30 M开始以1:3连续稀释,重复三次,整个实验在一天内完成。最后,()-PHCCC值对VU 0364439的百分比为102.3。()-PHCCC的百分比通过VU 0364439引发的最大反应除以同一天对照组PAM、()-PHCCC的反应值计算得出。实验也发现VU 0364439对人mGlu4的EC50值为19.8 nM[4]。
VU 0364439具有比理想值稍差的药代动力学特性。VU0364439的这种特性防止了VU0364439本身被用于体内操作,但是VU 0364439可为mGlu4提供更多的体外工具化合物[4]。
参考文献:
[1]. Lucyna Pomierny-Chamioo, 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.
Description | VU 0364439是代谢型谷氨酸受体-4(mGluR-4)的正向变构调节剂(PAM),对人mGluR-4的EC50值为19.8 nM。 | |||||
靶点 | human mGluR-4 | |||||
IC50 | 19.8 nM (EC50) |