详情描述
AZD7545 is a selective inhibitor of PDHK2 PDH kinase2 with IC50s of 368 nM and 64 nM for PDHK1 and PDHK2 respectively
Product information
CAS Number: 252017-04-2
Molecular Weight: 478.87
Formula: C19H18ClF3N2O5S
Chemical Name: 4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide
Smiles: C[C@@](O)(C(=O)NC1=CC=C(C=C1Cl)S(=O)(=O)C1C=CC(=CC=1)C(=O)N(C)C)C(F)(F)F
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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO: 95 mg/mL(198.38 mM).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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:
- Tuganova A, et al. Biochemistry. 2007, 46(29), 8592-8602.
- Mayers RM, et al. Biochem Soc Trans. 2003, 31(Pt 6), 1165-1167.
- Morrell JA, et al. Biochem Soc Trans. 2003, 31(Pt 6), 1168-1170.
Products are for research use only. Not for human use.