Home>>Signaling Pathways>> Proteases>> Endogenous Metabolite>>PF-07238025

PF-07238025

目录号 : GC71322

PF-07238025是BCKDC激酶(BDK)抑制剂(EC50=19 nM)。

PF-07238025 Chemical Structure

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1 mg
¥1,665.00
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5 mg
¥3,330.00
现货
10 mg
¥5,706.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

PF-07238025 is a BCKDC kinase (BDK) inhibitor (EC50=19 nM). PF-07238025 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-07238025 improved cardiometabolic endpoints and improves glucose tolerance in mice.

PF-07238025 (0.2-6 μM; 48 h) reduces pBCKDH in a dose-dependent manner in Hek293 cells, and increases BDK accumulation by 50%[1].

PF-07238025 (20 mg/kg, 100 mg/kg; 8 weeks) reduces glucose excursion after 2 days in HFD-fed mice, and leads significant reduction in both BCAAs and BCKAs by day 7[1].

References:
[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.

Chemical Properties

Cas No. SDF
分子式 C19H18N2O3S 分子量 354.42
溶解度 DMSO : 100 mg/mL (282.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) 储存条件 -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.8215 mL 14.1076 mL 28.2151 mL
5 mM 0.5643 mL 2.8215 mL 5.643 mL
10 mM 0.2822 mL 1.4108 mL 2.8215 mL
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