| 中文名称 |
VU 0364439
|
| 中文别名 |
N-[3-氯-4-[[(2-氯苯基)氨基]磺酰基]苯基]-2-吡啶甲酰胺;VU0364439 抑制剂
|
| 英文名称 |
VU 0364439
|
| 英文别名 |
VU0364439;N-[3-chloro-4-[(2-chlorophenyl)sulfamoyl]phenyl]pyridine-2-carboxamide;2-Pyridinecarboxamide (N-[3-chloro-4-[[(2-chlorophenyl)amino]sulfonyl]phenyl];CS-1000;VU-0364439;VU 0364439
|
| Cas No. |
1246086-78-1
|
| 分子式 |
C18H13N3O3Scl2
|
| 分子量 |
422.29
|
| 包装储存 |
Powder -20°C 3 years;4°C 2 years
|
| 详情描述 |
VU 0364439是mGlu4阳性变构调节剂(PAM),EC50为19.8 nM。
|
| 产品详情 |
VU 0364439是mGlu4阳性变构调节剂(PAM),EC50为19.8 nM。
|
| 生物活性 |
VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM.
IC50 Value: 19.8 nM(EC50)
Target: mGluR
in vitro:
in vivo: VU 0364439 possess less than ideal PK properties preventing their use as in vivo tools. It shows better stability in HLM (63% remaining) than RLM (2% remaining).
|
| 性状 |
Solid
|
| IC50 & Target[1][2] |
mGlu4 Receptor 19.8 nM (EC50)
|
| 运输条件 |
Room temperature in continental US; may vary elsewhere.
|
| 储存方式 |
Powder -20°C 3 years;4°C 2 years
|
| 参考文献 |
[1]. Hong, Sang-Phyo; Liu, Kevin G.; Ma, Gil et al. Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators. Journal of Medicinal Chemistry (2011), 54(14), 5070-5081.[2]. Engers, Darren W.; Gentry, Patrick R.; Williams, Richard et al. Synthesis and SAR of novel 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorganic & Medicinal Chem
|
| 溶解度数据 |
In Vitro: DMSO : 50 mg/mL (118.40 mM; Need ultrasonic)配制储备液
|
[1]. Hong, Sang-Phyo; Liu, Kevin G.; Ma, Gil et al. Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators. Journal of Medicinal Chemistry (2011), 54(14), 5070-5081.[2]. Engers, Darren W.; Gentry, Patrick R.; Williams, Richard et al. Synthesis and SAR of novel 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorganic & Medicinal Chem
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。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。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。