CAS: 188591-46-0; 4-Chloro-N-(2-((5-(Trifluoromethyl)Pyridin-2-yl)Sulfonyl)Ethyl)Benzamide

该化合物是某些酶的选择性抑制剂,特别是那些参与调制炎症途径的酶;该化合物展示了针对特定生物过程的具体行动机制,使其在药物开发领域,特别是针对与炎症和自发性疾病有关的情况.GSK-3787的特点是其独特的分子结构,有助于其生物活动和选择性.在物理特性方面,该化合物一般在室内温度上是固体,在各种有机溶剂中是可溶解的.与任何化学物质一样,安全和处理预防措施对于减轻与接触有关的潜在风险至关重要.正在进行的研究继续探索其在临床环境中的功效和安全状况,目的是确立其在治疗疗法中的作用.

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欧盟法规

ECHA物质C&L通报

上下游产品

4-chloro-benzoyl chloride

合成工艺路线路线简述

    📜2-((5-(Trifluoromethyl)Pyridin-2-yl)Sulfonyl)Ethanaminium Chloride,4-氯苯甲酰氯置于三乙胺体系中,用 二氯甲烷 用作溶剂,以4.25 G的收率获得4-氯-N-[2-[[5-(三氟甲基)-2-吡啶基]磺酰基]乙基]-苯甲酰胺
    参考文献:Identification And Characterization Of 4-Chloro-N-(2-{[5-Trifluoromethyl)-2-Pyridyl]Sulfonyl}Ethyl)Benzamide (Gsk3787),A Selective And Irreversible Peroxisome Proliferator-Activated Receptor δ (Pparδ) Antagonist
    标题:Identification And Characterization Of 4-Chloro-N-(2-{[5-Trifluoromethyl)-2-Pyridyl]Sulfonyl}Ethyl)Benzamide (Gsk3787),A Selective And Irreversible Peroxisome Proliferator-Activated Receptor δ (Pparδ) Antagonist
    摘要:4-Chloro-N-(2-{[5-Trifluoromethyl)-2-Pyridyl]Sulfonyl}Ethyl)Benzamide 3 (Gsk3787) Was Identified As A Potent And Selective Ligand For Ppar Delta Wish Good Pharmacokinetic Properties. A Detailed Binding Study Using Mass Spectral Analysis Confirmed Covalent Binding To Cys249 Within The Ppar Delta Binding Pocket. Gene Expression Studies Showed That Pyridylsulfone 3 Antagonized The Transcriptional Activity Of Ppar Delta And Inhibited Basal Cpt1A Gene Transcription. Compound 3 Is A Ppar Delta Antagonist With Utility As It Tool To Elucidate Ppar Delta Cell Biology And Pharmacology.
    Doi:10.1021/jm900464J

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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Gu Y, Li X, He T, Jiang Z, Hao P, Tang X. The Antifibrosis Effects of Peroxisome Proliferator-Activated Receptor δ on Rat Corneal Wound Healing after Excimer Laser Keratectomy. PPAR Res. 2014;2014:464935. doi: 10.1155/2014/464935. Epub 2014 Nov 13.
    2: Zhou X, Ringseis R, Wen G, Eder K. Carnitine transporter OCTN2 and carnitine uptake in bovine kidney cells is regulated by peroxisome proliferator-activated receptor β/δ. Acta Vet Scand. 2014 Apr 9;56:21. doi: 10.1186/1751-0147-56-21.
    3: Luo G, Shi Y, Zhang J, Mu Q, Qin L, Zheng L, Feng Y, Berggren-Söderlund M, Nilsson-Ehle P, Zhang X, Xu N. Palmitic acid suppresses apolipoprotein M gene expression via the pathway of PPARβ/δ in HepG2 cells. Biochem Biophys Res Commun. 2014 Feb 28;445(1):203-7. doi: 10.1016/j.bbrc.2014.01.170. Epub 2014 Feb 4. doi: 10.1371/journal.pone.0069702. Print 2013.

    合成参考文献


    参考文献:10.1016/j.taap.2021.115653
    摘要:Venezia O, Islam S, Cho C, Timme-Laragy AR, Sant KE. Modulation of PPAR signaling disrupts pancreas development in the zebrafish, Danio rerio. Toxicology and Applied Pharmacology. 2021 Sep;426():115653. doi: 10.1016/j.taap.2021.115653.
    参考文献:10.1021/jm900464j
    摘要:Shearer BG, Wiethe RW, Ashe A, Billin AN, Way JM, Stanley TB, Wagner CD, Xu RX, Leesnitzer LM, Merrihew RV, Shearer TW, Jeune MR, Ulrich JC, Willson TM. Identification and characterization of 4-chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide (GSK3787), a selective and irreversible peroxisome proliferator-activated receptor delta (PPARdelta) antagonist. J Med Chem. 2010 Feb 25;53(4):1857–61. doi: 10.1021/jm900464j.
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