apolipoprotein a-1

COG 133 TFA 是载脂蛋白 E (Apolipoprotein E, APOE) 肽的片段。COG 133 与 ApoE 全息蛋白竞争结合 LDL 受体，具有有效的抗炎和神经保护作用。COG 133 TFA 也是nAChR 拮抗剂，IC50为 445 nM。

ABCA1 inducer 1 是一种促进ABCA1表达的非脂质诱导剂。在携带人类APOE 3 4 基因的 E3 4FAD 小鼠中，该化合物提高了ABCA1的水平，增强了载脂蛋白 (APOE) 的脂质化作用，并有效逆转了多种阿尔茨海默病 (AD) 的表型，同时不会导致甘油三酯水平上升。

APOL1-IN-1是一种有效的载脂蛋白 L1(APOL1) 的抑制剂，可用于研究局灶节段性肾小球硬化 (FSGS) 和非糖尿病肾病 (NDKD) 的发病原理，促进对此类疾病的研究。

BMS-309403 sodium 是一种有效的选择性脂肪细胞脂肪酸结合蛋白aFABP, 也称为FABP4，aP2抑制剂，对 FABP4，FABP3 和 FABP5 的Ki 分别为 <2 nM，250 nM，350 nM。BMS-309403 sodium 与蛋白质内部的脂肪酸结合口袋相互作用，竞争性地抑制内源性脂肪酸的结合。BMS-309403 sodium 可改善载脂蛋白E 缺乏症小鼠和培养的人内皮细胞的内皮功能。

LVGRQLEEFL (mouse) TFA，即G*肽，对应[113,122]apoJ中的第113至122位氨基酸序列，表现出抗炎与抗动脉粥样硬化的特性。该肽能够整合至apoJ模拟物，生成HM-10 10肽，一种新型嵌合高密度脂蛋白模拟肽。HM-10 10肽能够保护视网膜色素上皮(RPE)及光感受器，防止氧化剂引起的细胞死亡。

apoB (4372-4392) 是有效的脂蛋白(a)组装抑制剂，IC50为40 μM，并能以高亲和力非共价结合载脂蛋白(a)。

Dihomo-γ-linolenic acid sodium (DGLA; all-cis-8,11,14-Eicosatrienoic acid) 是一种具有抗炎和抗增殖活性的 20 碳 ω-6 脂肪酸。Dihomo-γ-linolenic acid (sodium) 能减轻载脂蛋白 E 缺陷小鼠模型的动脉粥样硬化。

Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988). Alaproclate is a selective serotonin reuptake inhibitor (SSRI).1,2 It inhibits depletion of serotonin (5-HT) induced by 4-methyl-α-ethyl-m-tyramine in rat cerebral cortex, hippocampus, hypothalamus, and striatum (EC50s = 18, 4, 8, and 12 mg kg, respectively).1 Alaproclate inhibits NMDA-evoked currents and depolarization-induced voltage-dependent potassium currents in rat hippocampal neurons (IC50s = 1.1 and 6.9 μM, respectively) and does not inhibit GABA-evoked currents when used at concentrations up to 100 μM.2 It increases sirtuin 1 (SIRT1) levels in N2a murine neuroblastoma cells expressing apolipoprotein E4 (ApoE4; IC50 = 2.3 μM) and in the hippocampus in the FXFAD-ApoE4 transgenic mouse model of Alzheimer's disease when administered at a dose of 20 mg kg twice daily.3 Alaproclate (40 mg kg) decreases immobility time in the forced swim test in rats, indicating antidepressant-like activity.4 References1. Michael, G.B., Eidam, C., Kadlec, K., et al. Increased MICs of gamithromycin and tildipirosin in the presence of the genes erm(42) and msr(E)-mph(E) for bovine Pasteurella multocida and Mannheimia haemolytica. Journal of Antimicrobial Chemotherapy 67(6), 1555-1557 (2012).2. Svensson, B.E., Werkman, T.R., and Rogawski, M.A. Alaproclate effects on voltage-dependent K+ channels and NMDA receptors: Studies in cultured rat hippocampal neurons and fibroblast cells transformed with Kv1.2 K+ channel cDNA. Neuropharmacology 33(6), 795-804 (1994).3. Campagna, J., Soilman, P., Jagodzinska, B., et al. A small molecule ApoE4-targeted therapeutic candidate that normalizes sirtuin 1 levels and improves cognition in an Alzheimer's disease mouse model. Sci. Rep. 8(1), 17574 (2018).4. Danysz, W.P., A., Kostowski, W., Malatynska, E., et al. Comparison of desipramine, amitriptyline, zimeldine and alaproclate in six animal models used to investigate antidepressant drugs. Pharmacol. Toxicol. 62(1), 42-50 (1988).

LVGRQLEEFL（mouse）即G*肽，为[113,122]apoJ中113至122位氨基酸序列。该化合物展现抗炎与抗动脉粥样硬化功能。将LVGRQLEEFL（mouse）整合至apoJ模拟物，可生成HM-10 10肽，此为一种模拟肽及新型嵌合高密度脂蛋白。HM-10 10肽能守护视网膜色素上皮（RPE）及光感受器，防止氧化剂诱导下的细胞死亡。