CAS: 452342-67-5; 4-(4-(3-(Pyridin-2-yl)-1H-Pyrazol-4-yl)Pyridin-2-yl)-N-(Tetrahydro-2H-Pyran-4-yl)Benzamide

该化合物是一种合成化合物,属于小分子抑制剂类别,专门设计用于瞄准和抑制某些蛋白质动脉,主要因其在癌症和其他涉及异常动脉活动的疾病相关研究中的作用而得到承认,该复合体展示了对其目标的高度特殊性,有助于其潜在的治疗应用.GW788388的特点是其分子结构,其中包括有利于其与生物目标互动的特定功能组.它通常在体外和活体中研究,以评估其功效和安全特征.与许多实验化合物一样,详细的药用动力学和药用动力学特性对于了解其在生物系统中的行为至关重要.研究人员经常探索其对细胞扩散,流行性病的影响,并提示评估其作为治疗剂的潜力的路径.然而,根据最新资料,GW788388仍然主要是一种研究工具,而不是经批准的药物.

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物理性质

MSDS等安全信息

上下游产品

2-溴-4-[3-(2-吡啶)-1H-吡唑-4-基]吡啶 2-Bromo-4-[3-(Pyridin-2-yl)-1H-Pyrazol-4-Yl]Pyridine 446880-81-5
4-[4-(3-Pyridin-2-Yl-1-Trityl-1H-Pyrazol-4-yl)Pyridin-2-Yl]Benzoic Acid 452343-18-9
2-溴-4-(3-(吡啶-2-基)-1-三苯甲游基-1H-吡唑-4-基)吡啶 2-Bromo-4-(3-(Pyridin-2-yl)-1-Trityl-1H-Pyrazol-4-yl)Pyridine 446880-83-7

合成工艺路线路线简述

    📜2-吡啶甲酸乙酯置于盐酸,Sodium Hydroxide,四(三苯基膦)钯,双(三甲基硅烷基)氨基钾,Sodium Carbonate,Potassium Carbonate,1-羟基苯并三唑,一水合肼,溶剂黄146,1-(3-二甲基氨基丙基)-3-乙基碳二亚胺体系中,用 四氢呋喃,甲醇,乙醇,N,N-二甲基甲酰胺,丙酮,甲苯 作为反应溶剂,化学反应 47.8H,反应生成 4-[4-[3-(吡啶-2-基)-1H-吡唑-4-基]吡啶-2-基]-N-(四氢吡喃-4-基)苯甲酰胺
    参考文献:Discovery Of 4-{4-[3-(Pyridin-2-yl)-1H-Pyrazol-4-Yl]Pyridin-2-Yl}-N-(Tetrahydro-2H-Pyran-4-yl)Benzamide (Gw788388): A Potent,Selective,And Orally Active Transforming Growth Factor-β Type I Receptor Inhibitor
    标题:Discovery Of 4-{4-[3-(Pyridin-2-yl)-1H-Pyrazol-4-Yl]Pyridin-2-Yl}-N-(Tetrahydro-2H-Pyran-4-yl)Benzamide (Gw788388): A Potent,Selective,And Orally Active Transforming Growth Factor-β Type I Receptor Inhibitor
    摘要:Inhibitors Of Transforming,Growth Factor Beta (Tgf-Beta) Type I Receptor (Alk5) Offer A Novel Approach For The Treatment Of Fibrotic Diseases Such As Renal,Hepatic,And Pulmonary Fibrosis. The Optimization Of A Novel Phenylpyridine Pyrazole Series (1A) Led To The Identification Of Potent,Selective,And Orally Active Alk5 Inhibitors. The Cellular Potency And Pharmacokinetics Profiles Of These Derivatives Were Improved And Several Compounds Presented Antifibrotic Activity When Orally Administered To Rats In An Acute Liver Model Of Dimethylnitrosamine-(Dmn-) Induced Expression Of Collagen Ia1 Mrna,A Major Gene Contributing To Excessive Extra Cellular Matrix Deposit. One Of The Most Potent Alk5 Inhibitors Identified In This Chemical Series,Compound 13D (Gw788388),Reduced The Expression Of Collagen Ia1 By 80% At A Dose Of I Mg/kg,Twice A Day (B.I.D.). This Compound Significantly Reduced The Expression Of Collagen Iai Mrna When Administered Orally At 10 Mg/kg Once A Day (U.I.D.) In A Model Of Puromycin Aminonucleoside-Induced Renal Fibrosis.
    DOI:10.1021/jm0509905

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    主要参考文献


    1: Wang Y, Jiang H, Chen Q, Guo F, Zhang B, Hu L, Huang X, Shen W, Gao J, Chen W, Xu W, Cai Z, Wei L, Li M. Myofibroblast-Targeting Extracellular Vesicles: A Promising Platform for Cardiac Fibrosis Drug Delivery. Biomater Res. 2025 Apr 11;29:0179. doi: 10.34133/bmr.0179.
    2: PLOS Neglected Tropical Diseases Editors. Retraction: Oral Administration of GW788388, an Inhibitor of Transforming Growth Factor Beta Signaling, Prevents Heart Fibrosis in Chagas Disease. PLoS Negl Trop Dis. 2024 Jul 23;18(7):e0012360. doi: 10.1371/journal.pntd.0012360.
    3: Das K, Basak M, Mahata T, Biswas S, Mukherjee S, Kumar P, Moniruzzaman M, Stewart A, Maity B. Cardiac RGS7 and RGS11 drive TGFβ1-dependent liver damage following chemotherapy exposure. FASEB J. 2023 Aug;37(8):e23064. doi: 10.1096/fj.202300094R. 39(4):1773-1793. doi: 10.1007/s10565-022-09783-5. Epub 2022 Dec 31.

    合成参考文献


    参考文献:10.1152/ajpheart.01048.2009
    摘要:Tan SM, Zhang Y, Connelly KA, Gilbert RE, Kelly DJ. Targeted inhibition of activin receptor-like kinase 5 signaling attenuates cardiac dysfunction following myocardial infarction. American Journal of Physiology-Heart and Circulatory Physiology. 2010 May;298(5):H1415–25. doi: 10.1152/ajpheart.01048.2009.
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