AZD7545
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
AZD7545是丙酮酸脱氢酶激酶2的选择性抑制剂（PDHK2），其IC50值为6.4 nM[1]。
PDH催化丙酮酸脱羧，将其转换为乙酰辅酶A。因而，该酶受PDHK调节。PDHK抑制剂被研发用于治疗2型糖尿病。AZD7545是PDHK2的选择性抑制剂。其对PDHK1和PDK2的IC50值分别为36.8 nM和6.4 nM。此外，对于重组人PDHK2，AZD7545可以增加PDH活性，其EC50值为5.2 nM。体内研究表明，给予AZD7545显著激活肝脏的PDH活性，并部分激活骨骼肌和心脏的PDH活性。在Zucker（fa/fa）大鼠中，10 mg/kg的AZD7545将肌肉PDH活性从61%提升至97%，并将肝脏PDH活性从33.5%提升至72.8%[1，2]。
参考文献：
[1] Morrell J A, Orme J, Butlin R J, et al. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochemical society transactions, 2003, 31(6): 1168-1170.
[2] Mayers R M, Butlin R J, Kilgour E, et al. AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats. Biochemical Society Transactions, 2003, 31(6): 1165-1167.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 478.87 |
| Cas No. | 252017-04-2 |
| Formula | C19H18ClF3N2O5S |
| Solubility | ≥21.85 mg/mL in DMSO; insoluble in H2O; ≥15.63 mg/mL in EtOH with ultrasonic |
| Chemical Name | 4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide |
| SDF | Download SDF |
| Canonical SMILES | CC(C(=O)NC1=C(C=C(C=C1)S(=O)(=O)C2=CC=C(C=C2)C(=O)N(C)C)Cl)(C(F)(F)F)O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。 |
| 激酶实验 [1]: | |
|
PDHK同工酶抑制试验 |
[33P]ATP与PDH 亚基E1的结合测定实验于30℃条件下、含有100 μM ATP 和 E2亚基的Mops-K+缓冲液中进行。全部采用重组人蛋白。化合物J，K，L是AZD7545的衍生物。 IC50值以平均数±标准差的形式呈现，观测次数标注在括号中。 |
| 动物实验 [2]: | |
|
动物模型 |
Wistar大鼠模型; 肥胖的(fa/fa) Zucker大鼠模型 |
|
剂量 |
3、10、和30 mg/kg；每天两次口服给药；持续7天 |
|
应用 |
在Wistar大鼠模型中，AZD7545更加有效地增加肝脏的PDH活性，而增加骨骼肌和心脏的PDH活性较弱；同时，在肥胖的(fa/fa) Zucker大鼠模型中，AZD7545显著地提高体内丙酮酸脱氢酶活并且有效地控制血糖。 |
|
注意事项 |
请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同，这是由实验系统的误差引起的，属于正常现象。 |
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References: 1. Morrell, J. A., Orme, J., Butlin, R. J., Roche, T. E., Mayers, R. M. and Kilgour, E. (2003) AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans. 31, 1168-1170 2. Mayers, R. M., Butlin, R. J., Kilgour, E., Leighton, B., Martin, D., Myatt, J., Orme, J. P. and Holloway, B. R. (2003) AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats. Biochem Soc Trans. 31, 1165-1167 | |
| Description | AZD7545是有效的PDHK抑制剂，对PDHK1和PDHK2的IC50值分别为36.8 nM和6.4 nM。 | |||||
| 靶点 | PDHK2 | PDHK1 | ||||
| IC50 | 6.4 nM | 36.8 nM | ||||
质量控制和MSDS
- 批次:
化学结构
