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CAS No.: 1301214-47-0

PF-05175157 Catalog No. CSN24313

Synonyms: PF-05175157

PF-05175157 is a potent and selective ACC inhibitor with IC50 values of 27nM and 33nM for ACC1 and ACC2, respectively.

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实验方案

技术信息

生物活性

描述Acetyl-CoA carboxylase (ACC) is a biotin carboxylase that catalyzes the ATP-dependent condensation of acetyl-CoA and carbonate to form malonyl-CoA. The malonyl-CoA is an essential and rate-limiting substrate for de novo lipogenesis (DNL), and it acts as an allosteric inhibitor of the enzyme carnitine-palmitoyl transferase I (CPT-1)^[1]. PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC₅₀ values of 27.0, 33.0, 23.5 and 50.4 nM for ACC1 (human), ACC2 (human), ACC1 (rat), ACC2 (rat), respectively^[2]. In the First-in-Human study, single ascending doses of PF-05175157 ranging from 10 to 800 mg were safe and well-tolerated. Fructose stimulated DNL was inhibited over this time course; peak fructose-stimulated fractional DNL was reduced by 63.6% (90% CI = 75.1–52.0%) relative to placebo treatment^[2]. PF-05175157 shows antiviral activities against West Nile virus (WNV) dengue virus (DENV) and Zika virus (ZIKV) with EC₅₀ values of 2.7 ± 1.3 µM, 1.0 ± 0.3 µM and < 1.2 µM, respectively^[3]. Murine model of WNV infection were treated with PF-05175157 (20 mg/kg) or drug vehicle twice a day p.o.. When compared to control animals, mice treated with PF-05175157 exhibited a significant decrease of viral load in plasma at 3 and 4 days after infection, a significant reduction in the amount of viral RNA in the kidney and a tendency for a reduction in the amount of viral RNA in the lung^[3].
参考文献

[1] Saggerson D. Malonyl-CoA, a key signaling molecule in mammalian cells. Annu Rev Nutr. 2008;28:253-72. doi: 10.1146/annurev.nutr.28.061807.155434. PMID: 18598135.
[2] Griffith DA, Kung DW, Esler WP, Amor PA, Bagley SW, Beysen C, Carvajal-Gonzalez S, Doran SD, Limberakis C, Mathiowetz AM, McPherson K, Price DA, Ravussin E, Sonnenberg GE, Southers JA, Sweet LJ, Turner SM, Vajdos FF. Decreasing the rate of metabolic ketone reduction in the discovery of a clinical acetyl-CoA carboxylase inhibitor for the treatment of diabetes. J Med Chem. 2014 Dec 26;57(24):10512-26. doi: 10.1021/jm5016022. Epub 2014 Dec 11. PMID: 25423286; PMCID: PMC4281100.
[3] Jiménez de Oya N, Esler WP, Huard K, El-Kattan AF, Karamanlidis G, Blázquez AB, Ramos-Ibeas P, Escribano-Romero E, Louloudes-Lázaro A, Casas J, Sobrino F, Hoehn K, James DE, Gutiérrez-Adán A, Saiz JC, Martín-Acebes MA. Targeting host metabolism by inhibition of acetyl-Coenzyme A carboxylase reduces flavivirus infection in mouse models. Emerg Microbes Infect. 2019;8(1):624-636. doi: 10.1080/22221751.2019.1604084. PMID: 30999821; PMCID: PMC6493301.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4661 mL
- 12.3307 mL
- 24.6614 mL
- 5 mM
- 0.4932 mL
- 2.4661 mL
- 4.9323 mL
- 10 mM
- 0.2466 mL
- 1.2331 mL
- 2.4661 mL

技术信息

CAS号

1301214-47-0

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H27N5O2

运输

蓝冰

分子量

405.49

别名

PF-05175157

溶解度

DMSO	15.0 mg/mL (37.0 mM)
Water	insoluble

动物实验配方

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