Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
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
50 mM
0.0418 mL
0.2088 mL
0.4176 mL
Description
AZD7545 is a potent inhibitor with IC50 of 36.8 nM and 6.4 nM for and , respectively. It failed to inhibit PDHK4 at higher concentrations(>10 nM), AZD7545 stimulates PDHK4 activity.
In the presence of recombinant human PDHK2, AZD7545 increases PDH activity with EC50 of 5.2 nM. In primary rat hepatocytes, AZD7545 increases PDH activity with EC50 of 105 nM. AZD7545 inhibits PDHK activity by disrupting the interactions between PDHK2 and the inner lipoyl-bearing domains (L2) of the dihydrolipoyl transacetylase component (E2) of PDC.
In vivo
In Wistar rats, AZD7545 increases the percentage of active PDH in the liver and skeletal muscle. In obese, insulin-resistant, Zucker rats, AZD7545 eliminates the postprandial elevation in blood glucose.
