AZD7545 is a potent PDHK inhibitor with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2, respectively. PDHK4 can not be inhibited at high concentrations, but can stimulate PDHK4 activity.

 

Brand: BCM

 

Target: Dehydrogenase

 

Signaling Pathways: Metabolism

 

In Vitro: In obese insulin-resistant Zucker rats,AZD7545 eliminated the postprandial rise in blood sugar. AZD7545 increased the percentage of active PDH in liver and skeletal muscle in Wistar rats.

 

In Vivo: AZD7545 inhibits PDHK activity by disrupting the interaction of PDHK2 with the internal lipoyl domain of the dihydrolipoic acetyltransferase component of PDC. AZD7545 increased PDH activity in primary rat hepatocytes with EC50 of 105 nM. In the presence of recombinant human PDHK2,AZD7545 increased PDH activity and EC50 was 5.2 nM.

 

Boiling Point: 683.1±55.0 °C(Predicted)

 

pKa: 10.39±0.29(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: C[C@@](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  

 

InChIKey: DTDZLJHKVNTQGZ-GOSISDBHSA-N  

 

InChI: InChI=1S/C19H18ClF3N2O5S/c1-18(28,19(21,22)23)17(27)24-15-9-8-13(10-14(15)20)31(29,30)12-6-4-11(5-7-12)16(26)25(2)3/h4-10,28H,1-3H3,(H,24,27)/t18-/m1/s1

 

Attribute
[Chem Name]	4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide
[Synonym]	AZD7545
[CAS No.]	252017-04-2
[MDL No.]	MFCD25976792
[Formula]	C19H18ClF3N2O5S
[Molecular]	478.87
[Form]	Solid Powder
[Storage]	Sealed in dry, 2-8°C

Goods Tag