产品
编 号：F293363
分子式：C19H18ClF3N2O5S
分子量：478.87
分子式：C19H18ClF3N2O5S
分子量：478.87
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规格
价格
是否有货
10mM*1mL in DMSO
询价
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5mg
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10mg
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25mg
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50mg
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100mg
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结构图
CAS No: 252017-04-2
产品详情
生物活性：
AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.
体内研究：
A single dose of AZD7545 (Oral administration; 10 mg/kg once a day (08:00 h) or Twice a day (08:00 and 18:00 h); for 7 days) to Wistar rats increases the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner. A single dose of 10 mg/kg also significantly elevates muscle PDH activity in obese Zucker (fa/fa) rats.Animal Model:Obese male (fa/fa) Zucker rats
Dosage:10 mg/kg
Administration:Oral administration; once a day (08:00 h) or Twice a day ( 08:00 and 18:00 h); for 7 days
Result:Improved the control of blood glucose levels.
体外研究：
AZD7545 (10 μM; 90 hours for BRAFV600E human melanoma cells and 120 hours for NRAS mut human melanoma cells) specifically suppresses growth of cells harboring BRAF and NRAS mutations as well as in inhibitor-resistant human melanoma.
AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.
体内研究：
A single dose of AZD7545 (Oral administration; 10 mg/kg once a day (08:00 h) or Twice a day (08:00 and 18:00 h); for 7 days) to Wistar rats increases the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner. A single dose of 10 mg/kg also significantly elevates muscle PDH activity in obese Zucker (fa/fa) rats.Animal Model:Obese male (fa/fa) Zucker rats
Dosage:10 mg/kg
Administration:Oral administration; once a day (08:00 h) or Twice a day ( 08:00 and 18:00 h); for 7 days
Result:Improved the control of blood glucose levels.
体外研究：
AZD7545 (10 μM; 90 hours for BRAFV600E human melanoma cells and 120 hours for NRAS mut human melanoma cells) specifically suppresses growth of cells harboring BRAF and NRAS mutations as well as in inhibitor-resistant human melanoma.
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