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

PF-07238025

Catalog No.GC71322 Copy One-Click Copy Product Info

PF-07238025는 BCKDC kinase (BDK) 억제제 (EC50=19 nM)이다.

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PF-07238025 Chemical Structure

Size 가격 재고 수량
1 mg
US$167.00
재고 있음
5 mg
US$333.00
재고 있음
10 mg
US$571.00
재고 있음

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고객 리뷰

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.



Description of PF-07238025

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 of PF-07238025

Cas No. SDF
Formula C19H18N2O3S M.Wt 354.42
Solubility 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) Storage -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of PF-07238025

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.8215 mL 14.1076 mL 28.2151 mL
5 mM 564.3 μL 2.8215 mL 5.643 mL
10 mM 282.2 μL 1.4108 mL 2.8215 mL
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In vivo Formulation Calculator (Clear solution) of PF-07238025

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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