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AZD7545 Sale

(Synonyms: 4-[[3-氯-4-[[(2R)-3,3,3-三氟-2-羟基-2-甲基-1-氧代丙基]氨基]苯基]磺酰基]-N,N-二甲基苯甲酰胺) 目录号 : GC13669

A PDK inhibitor

AZD7545 Chemical Structure

Cas No.:252017-04-2

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,827.00
现货
5mg
¥1,302.00
现货
10mg
¥2,100.00
现货
50mg
¥4,799.00
现货
100mg
¥7,959.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

Inhibition of PDHK isoenzyme assay

The incorporation of [33P]ATP into the E1 subunit of PDH is measured at 30°C in Mops-K+ buffer in the presence of 100 μM ATP and E2 subunit. Recombinant human proteins are used throughout. Compounds J, K and L are from the same chemical series as AZD7545. IC50 values are means±.E.M. with the number of observations given in parentheses.

Animal experiment [2]:

Animal models

Wistar rats model; obese Zucker (fa/fa) rats model

Dosage form

3, 10, and 30 mg/kg twice daily;oral administration for 7 days

Applications

AZD7545 more effectively increased PDH activity in liver than in skeletal muscle and heart in wistar rats model. Moreover, AZD7545 significantly elevated pyruvate dehydrogenase (PDH) activity in vivo and markedly improved blood glucose control in obese (fa/fa) Zucker rats.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

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

产品描述

AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) with IC50 value of 6.4nM [1].

PDH catalyzes the decarboxylation of pyruvate, converting it to acetyl-CoA. This enzyme is regulated by PDH kinases. The inhibitor of PDHK is developed for the treatment of type 2 diabetes. AZD7545 is a selective inhibitor of PDHK2. It inhibits PDHK1 and PDHK2 with IC50 values of 36.8nM and 6.4nM, respectively. Besides that, AZD7545 increases PDH activity with EC50 value of 5.2nM when using recombinant human PDHK2. In vivo studies show that administration of AZD7545 significantly activates PDH activity in liver and partially activates PDH activity in skeletal muscle and heart. In Zucker (fa/fa) rats, AZD7545 at dose of 10 mg/kg increases muscle PDH from 61% to 97% active and liver PDH from 33.5% to 72.8% [1, 2].

References:
[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.

Chemical Properties

Cas No. 252017-04-2 SDF
别名 4-[[3-氯-4-[[(2R)-3,3,3-三氟-2-羟基-2-甲基-1-氧代丙基]氨基]苯基]磺酰基]-N,N-二甲基苯甲酰胺
化学名 4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide
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
分子式 C19H18ClF3N2O5S 分子量 478.87
溶解度 ≥ 21.85mg/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。
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。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.0882 mL 10.4412 mL 20.8825 mL
5 mM 0.4176 mL 2.0882 mL 4.1765 mL
10 mM 0.2088 mL 1.0441 mL 2.0882 mL
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