| Bioactivity | PF-07247685 is a BCKDC kinase (BDK) inhibitor (EC50=2.2 nM). PF-07247685 stabilizes the interaction between BDK and BCKDH core subunit E2 and prevents phosphorylation of E1. While BDK mediates branched-chain ketoacid dehydrogenase (BCKDH) phosphorylation, and inhibition of BCKDH is involved in controlling the rate-limiting step of branched-chain amino acid (BCAA) degradation. Impaired BCAA catabolism has been associated with several diseases, particularly cardiometabolic diseases, including heart failure (HF), type 2 diabetes mellitus (T2DM), non-alcoholic fatty liver disease (NAFLD), and obesity. PF-07247685 improved cardiometabolic endpoints and improves glucose tolerance in mice[1]. |
| Target | EC50: 2.2 nM (BCKDC kinase, BDK) |
| Invitro | PF-07247685 (0.01-0.3 μM；48 h) 在 Hek293 细胞中以剂量依赖性方式减少 pBCKDH，并使 BDK 积累增加 50%[1]。 0 --> PF-07247685 相关抗体: |
| In Vivo | PF-07247685（10 mg/kg、100 mg/kg；每天两次，持续 18 天）可显着改善 HFD 喂养小鼠的葡萄糖耐量并降低组织 BCAA/BCKA[1]。 |
| Name | PF-07247685 |
| Formula | C21H20N2O3S |
| Molar Mass | 380.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Roth Flach RJ, et al. Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels. Nat Commun. 2023 Aug 9;14(1):4812. |