Dichloro(bipyridine)platinum 是一种强效的铂类抗肿瘤配合物,是顺铂(Cisplatin)的结构类似物。它通过联吡啶配体增强分子的脂溶性和平面堆积能力。该化合物通过与 DNA 发生共价结合或嵌入式结合,形成顺式-Pt-DNA 加合物,从而干扰 DNA 复制和转录过程。研究表明,该类配合物能有效激活促凋亡信号通路,对多种耐药性肿瘤细胞系具有显著的生长抑制作用,是开发新型金属抗癌药物的重要基础分子。
NBI-30545 is a potent corticotropin-releasing factor-1 antagonist with sufficient lipophilicity and water solubility for the treatment of stress disorders.
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from thesn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.1CAY10641 is an inactive alcohol derivative of a highly potent (IC50= 12 nM) cPLA2α inhibitor.2The parent compound demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.2CAY10641 is rapidly cleared from the blood stream (only 0.5 μg/ml remains 30 minutes after 10 mg/kg intravenous administration to mice).2However, no other biological effects have been reported.
1.Schaloske, R.H., and Dennis, E.A.The phospholipase A2 superfamily and its group numbering systemBiochemica et Biophysica Acta17611246-1259(2006) 2.Drews, A., Bovens, S., Roebrock, K., et al.1-(5-carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α with reduced lipophilicity: Synthesis, biological activity, metabolic stability, solubility, bioavailability, and topical in vivo activityJournal of Medicinal Chemistry535165-5178(2010)
AZD6642 is a potential and selective 5-Lipoxygenase activating Protein (FLAP) inhibitor. AZD6642 shows high specific potency and low lipophilicity resulting in a selective and metabolically stable profile. Based on initial PK/PD relations a low dose to human was predicted.
Sodium ionophore VI 是一种具有高选择性的钠离子载体,广泛用于阳离子光学传感器的开发。该化合物具有极强的亲脂性,能够作为中性载体嵌入聚合物膜(如 PVC 膜)中,并与特定的亲脂性阴离子染料(如荧光素衍生物)配合使用。通过在膜界面介导钠离子的选择性交换,Sodium ionophore VI 可将离子浓度的变化转化为光学信号,实现在复杂生物或环境样品中对钠离子、钾离子及铵离子的监测。