5.33639

Pyruvate Dehydrogenase Kinase Inhibitor, AZD7545

• 同義詞: Pyruvate Dehydrogenase Kinase Inhibitor, AZD7545, PDK Inhibitor, ( R)-4-(3-Chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenylsulfonyl)-N,N-dimethylbenzamide, PDh Kinase Inhibitor, PDhK Inhibitor
• 經驗公式（希爾表示法）: C₁₉H₁₈ClF₃N₂O₅S
• CAS號碼: 252017-04-2
• 分子量：: 478.87
• MDL號碼: MFCD25976792
• 分類程式碼代碼: 12352200
• NACRES: NA.77

屬性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white
• 溶解度: DMSO: 50 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: FC(F)(F)[C@@](O)(C)C(=O)Nc1c(cc(cc1)[S](=O)(=O)c2ccc(cc2)C(=O)N(C)C)Cl
• 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
• InChI 密鑰: DTDZLJHKVNTQGZ-GOSISDBHSA-N

描述

一般說明

A cell-permeable, bioavailable trifluomethylpropanamide compound that acts as a potent, selective, reversible, non-ATP-competitive inhibitor of pyruvate dehydrogenase kinases (IC₅₀ = 36.8 & 6.4 nM for PDhK1 & PDhK2, respectively). Inhibits PDhK3 at much higher concentrations (IC₅₀ = 600 nM) and robustly stimulates PDhK4 activity (>10 nM). Also shown to increase pyruvate dehydrogenase (PDh) activity in liver and muscle, and potentiates pyruvate oxidation (EC₅₀ = 105 nM in rat hepatocytes). Occupies lipoyl domain-binding site of PDhK2 (K_d = 19.2 nM) and disrupts the association of PDhK2 and inner lipoyl-bearing domain 2 of dihydrolipoyl acetyltransferase. Improves 24-h glucose profile and eliminates postparandial elevation in blood glucose in Zucker (fa/Fa) rats (10 mg/kg, b.i.d, p.o.,7 days).

A cell-permeable, bioavailable trifluomethylpropanamide compound that acts as a potent, selective, reversible, non-ATP-competitive inhibitor of pyruvate dehydrogenase kinases (IC₅₀ = 36.8 & 6.4 nM for PDhK1 & PDhK2, respectively). Inhibits PDhK3 at much higher concentrations (IC₅₀ = 600 nM) and robustly stimulates PDhK4 activity (>10 nM). Also shown to increase pyruvate dehydrogenase (PDh) activity in liver and muscle, and potentiates pyruvate oxidation (EC₅₀ = 105 nM in rat hepatocytes). Occupies lipoyl domain-binding site of PDhK2 (K_d = 19.2 nM) and disrupts the association of PDhK2 and inner lipoyl-bearing domain 2 of dihydrolipoyl acetyltransferase. Improves 24-h glucose profile and eliminates postparandial elevation in blood glucose in Zucker (fa/Fa) rats (10 mg/kg, b.i.d, p.o.,7 days).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

Pyruvate Dehydrogenase Kinase Inhibitor, AZD7545, CAS 252017-04-2, is a potent, selective, reversible inhibitor of PDHK2 (IC₅₀ = 6.4 nM). Inhibits PDHK1 at higher levels (IC₅₀ = 36.8 nM).

生化／生理作用

Cell permeable: yes

Primary Target
pyruvate dehydrogenase kinases

Target IC₅₀: 36.8 & 6.4 nM for PDhK1 & PDhK2, respectively

警告

Toxicity: Standard Handling (A)

重構

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他說明

Li, J., et al. 2009. J. Biol. Chem.284, 34458.
Tuganova, A., et al. 2007. Biochemistry46, 8592.
Morrell, J.A., et al. 2003. Biochem. Soc. Trans.31, 1168.
Mayers, R.M., et al. 2003. Biochem. Soc. Trans.31, 1165.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable