| CAS NO: | 252017-04-2 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 2mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| Molecular Weight (MW) | 478.87 |
|---|---|
| Formula | C19H18ClF3N2O5S |
| CAS No. | 252017-04-2 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 95 mg/mL (198.4 mM) |
| Water: <1 mg/mL | |
| Ethanol: 95 mg/mL (198.4 mM) | |
| Other Info | Exact Mass: 478.0577 Chemical Name: 4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamideSMILES Code: 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 |
| Synonyms | AZD-7545; AZD 7545; AZD7545; 4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide |
| In Vitro | In vitro 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. Kinase Assay: AZD7545 is a selective inhibitor of PDHK2. It inhibits PDHK1 and PDHK2 with IC50 values of 36.8nM and 6.4nM, respectively. Besides that, AZD7545 increases PDH activity with EC50 value of 5.2nM when using recombinant human PDHK2. Cell Assay: In rat hepatocytes, the rate of pyruvate oxidation was stimulated 2-fold (EC(50) 105 nM) [2]. in vivo: A single dose of AZD7545 to Wistar rats increased the proportion of liver PDH in its active, dephosphorylated form in a dose-related manner from 24.7 to 70.3% at 30 mg/kg; and in skeletal muscle from 21.1 to 53.3%. A single dose of 10 mg/kg also significantly elevated muscle PDH activity in obese Zucker (fa/fa) rats. |
|---|---|
| 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. |
| Animal model | In vivo studies show that administration of AZD7545 significantly activates PDH activity in liver and partially activates PDH activity in skeletal muscle and heart. In Zucker (fa/fa) rats, AZD7545 at dose of 10 mg/kg increases muscle PDH from 61% to 97% active and liver PDH from 33.5% to 72.8%. |
| Formulation & Dosage | 10 mg/kg |
| References | Biochem Soc Trans. 2003 Dec;31(Pt 6):1165-7; Biochemistry. 2007 Jul 24;46(29):8592-602. |
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