Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-07247685, a potent BCKDC kinase (BDK) inhibitor (EC 50 = 2.2 nM), enhances the binding between BDK and the BCKDH E2 core subunit to block E1 phosphorylation. BDK regulation is crucial for BCKDH activity, which manages the rate-limiting step in the catabolism of branched-chain amino acids (BCAA). Dysfunctional BCAA metabolism is linked to various cardiometabolic disorders such as heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 has demonstrated an ability to improve cardiometabolic parameters and glucose tolerance in mice [1].
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Description | PF-07247685, a potent BCKDC kinase (BDK) inhibitor (EC 50 = 2.2 nM), enhances the binding between BDK and the BCKDH E2 core subunit to block E1 phosphorylation. BDK regulation is crucial for BCKDH activity, which manages the rate-limiting step in the catabolism of branched-chain amino acids (BCAA). Dysfunctional BCAA metabolism is linked to various cardiometabolic disorders such as heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 has demonstrated an ability to improve cardiometabolic parameters and glucose tolerance in mice [1]. |
In vitro | PF-07247685 (0.01-0.3 μM; 48 h) reduces pBCKDH in a dose-dependent manner and increases BDK accumulation by 50% in Hek293 cells [1]. |
In vivo | PF-07247685 (dosed at 10 mg/kg, 100 mg/kg; twice daily for 18 days) significantly improved glucose tolerance and reduced tissue BCAA/BCKA [1] in mice fed a high-fat diet (HFD). |
Molecular Weight | 380.46 |
Formula | C21H20N2O3S |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
You can also refer to dose conversion for different animals. More
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PF-07247685 Metabolism Endogenous Metabolite inhibitor inhibit