4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethylbenzamide
AZD7545
CAS: 252017-04-2
Molecular Formula: C19H18ClF3N2O5S
4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethylbenzamide - Names and Identifiers
| Name | AZD7545 |
| Synonyms | AZD7545 AZD4575 AZD7547 CS-1842 AZD 7547 AZD-7547 4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethylbenzamide |
| CAS | 252017-04-2 |
4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethylbenzamide - Physico-chemical Properties
| Molecular Formula | C19H18ClF3N2O5S |
| Molar Mass | 478.87 |
| Density | 1.473±0.06 g/cm3(Predicted) |
| Boling Point | 683.1±55.0 °C(Predicted) |
| Solubility | DMSO: ≥ 46 mg/mL |
| pKa | 10.39±0.29(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | AZD7545 increases PDH activity in the presence of recombinant human PDHK2 with an EC50 of 5.2 nM. AZD7545 increases PDH activity in primary rat hepatocytes with an EC50 of 105 nM. AZD7545 inhibits PDHK activity by disrupting the interaction of PDHK2 with the internal thiooctanoyl domain (L2) of the dihydrolipoic acid acetyltransferase component (E2) of PDC. |
| In vivo study | In Wistar rats, AZD7545 increases the percentage of active PDH in liver and skeletal muscle. In obese, insulin-resistant Zuker rats, AZD7545 abolished the rise in postprandial blood glucose. |
4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethylbenzamide - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.088 ml | 10.441 ml | 20.883 ml |
| 5 mM | 0.418 ml | 2.088 ml | 4.177 ml |
| 10 mM | 0.209 ml | 1.044 ml | 2.088 ml |
| 5 mM | 0.042 ml | 0.209 ml | 0.418 ml |
Last Update：2024-01-02 23:10:35
4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethylbenzamide - Reference Information
| biological activity | AZD7545 is a potent PDHK inhibitor with an IC50 of 36.8 nM and 6.4 nM for PDHK1 and PDHK2, respectively. PDHK4 cannot be inhibited at high concentrations, which can stimulate PDHK4 activity. |
| Target | TargetValue PDHK2 6.4 nM PDHK1 36.8 nM |
| Target | Value |
| PDHK2 | 6.4 nM |
| PDHK1 | 36.8 nM |
| in vitro study | in the presence of recombinant human PDHK2, AZD7545 increased PDH activity with an EC50 of 5.2 nM. AZD7545 increases PDH activity in primary rat hepatocytes with an EC50 of 105 nM. AZD7545 inhibits PDHK activity by disrupting the interaction of PDHK2 with the internal thiooctanoyl domain (L2) of the dihydrolipoic acid acetyltransferase component (E2) of PDC. |
| in vivo study | in Wistar rats, AZD7545 increased the percentage of active PDH in liver and skeletal muscle. In obese, insulin-resistant Zuker rats, AZD7545 abolished the rise in postprandial blood glucose. |
Last Update：2024-04-10 22:29:15
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Spot supply
Product Name: AZD7545 Visit Supplier Webpage Request for quotationCAS: 252017-04-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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4-[[3-Chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methyl-1-oxopropyl]amino]phenyl]sulfonyl]-N,N-dimethylbenzamide
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