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Submit ReviewPF 06424439
说明： Potent and selective DGAT2 inhibitor
化学名： [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinylmethanone methanesulfonate
纯度： ≥98% (HPLC)
生物活性 for PF 06424439
PF 06424439 is a potent and selective DGAT2 inhibitor (IC50 = 14 nM). Exhibits no significant activity at MGAT1-3 or DGAT1. Reduces triglyderide synthesis in human hepatocytes in vitro. Reduces plasma triglyceride and cholesterol levels in a rat dyslipidemia model. Orally bioavailable.
许可信息
Sold for research purposes under agreement from Pfizer Inc.
技术数据 for PF 06424439
| 分子量 | 536.05 |
| 公式 | C22H26ClN7O.CH4O3S |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 1469284-79-4 |
| PubChem ID | 89854212 |
| InChI Key | ZSTFDNQQOJUJFL-XFULWGLBSA-N |
| Smiles | ClC(C=N1)=CN1C2(CC2)C3=NC4=CC=C(N5C[C@H](C(N6CCCC6)=O)CCC5)N=C4N3.O=S(C)(O)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for PF 06424439
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 53.6 | 100 | |
| DMSO | 53.6 | 100 |
制备储备液 for PF 06424439
以下数据基于产品分子量 536.05。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.87 mL | 9.33 mL | 18.65 mL |
| 5 mM | 0.37 mL | 1.87 mL | 3.73 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.87 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.37 mL |
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产品说明书 for PF 06424439
参考文献 for PF 06424439
参考文献是支持产品生物活性的出版物。
Futatsugi et al (2015) Discovery and optimization of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2). J.Med.Chem. 58 7173 PMID: 26349027
If you know of a relevant reference for PF 06424439, please let us know.
按产品操作查看相关产品
关键词: PF 06424439, PF 06424439 supplier, PF06424439, diacylglyercol, O-Acyltransferases, DGAT2, inhibitors, inhibits, potent, selective, orally, bioavailable, dyslipidemia, Diacylglycerol, O-Acyltransferase, 6348, Tocris Bioscience
4 篇 PF 06424439 的引用文献
引用文献是使用了 Tocris 产品的出版物。 PF 06424439 的部分引用包括：
Jian et al (2020) ABHD5 suppresses cancer cell anabolism through lipolysis-dependent activation of the AMPK/mTORC1 pathway. J Biol Chem 296 100104 PMID: 33219129
Kai et al (2021) BATF Regulates T Regulatory Cell Functional Specification and Fitness of Triglyceride Metabolism in Restraining Allergic Responses. J Immunol 206 2088-2100 PMID: 33879580
Naomi P et al (2023) An AI-guided screen identifies probucol as an enhancer of mitophagy through modulation of lipid droplets. PLoS Biol 21 e3001977 PMID: 36862640
Soeren S et al (2022) Reducing lipid bilayer stress by monounsaturated fatty acids protects renal proximal tubules in diabetes. Elife 11 PMID: 35550039
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PF 06424439 的评论
平均评分: 5 (Based on 1 Review.)
Have you used PF 06424439?
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Works great!.
By
Qing Li on 10/19/2022
分析类型： In Vitro
种属： Mouse
细胞系/组织： BMDM
I incubated BMDM with this inhibitor, it reduced the lipid level. Works great!
