[CAS NO. 252017-04-2] AZD7545

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [252017-04-2]

Catalog

SLK-S7517

Brand

Selleck

CAS

252017-04-2

DESCRIPTION [252017-04-2]

Overview

MDL	MFCD25976792
Molecular Weight	478.87
Molecular Formula	C19H18ClF3N2O5S
SMILES	O=C(N(C)C)C1=CC=C(S(=O)(C2=CC=C(NC([C@@](C)(O)C(F)(F)F)=O)C(Cl)=C2)=O)C=C1

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	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.

Targets

PDHK2 ^[1]	PDHK1 ^[1]
6.4 nM	36.8 nM

In vitro

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.

References

[1] Morrell JA, et al. Biochem Soc Trans. 2003, 31(Pt 6), 1168-1170.
[2] Mayers RM, et al. Biochem Soc Trans. 2003, 31(Pt 6), 1165-1167.
[3] Tuganova A, et al. Biochemistry. 2007, 46(29), 8592-8602.