lipoprotein ldl

是胆固醇酯转移蛋白 (CETP) 选择性抑制剂。根据人血浆的抑制曲线，Torcetrapib (CP-529414) 对CETP 的最有效浓度为 37 nM。

Atorvastatin Sodium (Lipitor) 是一种HMG-CoA 还原酶的竞争性抑制剂，增加肝细胞上低密度脂蛋白（LDL）受体的表达。Atorvastatin sodium 处理抑制水汽蛋白4来减轻缺血性脑水肿。

Ro 48-8071 fumarate 是一种氧化鲨烯环化酶抑制剂(IC50:6.5 nM)。

Gemcabene calcium , a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) andexerting anti-inflammatory activity, lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP).

PCSK9-IN-29 是一种有效的降脂药物。在 hepG2 细胞中，该化合物能够增强低密度脂蛋白受体 (LDLR) 的表达，同时减少 PCSK9 蛋白的表达。此外，在食用高脂肪饮食的食蟹猴体内，PCSK9-IN-29 能显著降低血清中 LDL-C、TC 以及肝酶 ALT 的水平，有效减轻体重和体脂，并提升骨矿物质含量。该化合物主要用于非酒精性脂肪性肝炎与肥胖症的研究领域。

PCSK9-IN-30（化合物3f）是一款有效的PCSK9抑制剂，其通过与PCSK9的隐性结合槽互作，阻止PCSK9与低密度脂蛋白受体 (LDLR) 的结合（IC50为537 nM），从而促进肝细胞重新吸收低密度脂蛋白 (LDL) 并下调血浆中的胆固醇水平。在小鼠体内的研究显示，PCSK9-IN-30具备良好的生物利用度，适合应用于心血管疾病的研究领域。

Oxidized low density lipoprotein (Human) (Human ox-LDL) 在动脉粥样硬化的形成中扮演关键角色。此化合物藉由细胞质衔接蛋白TRAF3IP2促使内皮功能发生障碍。此外，Oxidized low density lipoprotein (Human) 能够刺激内皮细胞的活化与粘附分子的产生，同时抑制eNOS活性和NO的生成。同时，它还能在巨噬细胞中激活NLRP3炎症小体。

MD-700, 一种新型异苯并呋喃酮，于0.03 microg ml浓度下能在4小时内提升HepG2细胞中的LDL受体表达。MD-700选择性降低LDL及极低密度脂蛋白胆固醇水平。

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

MK-8262, an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor (IC 50 = 53 nM, log D = 5.3), is a bistrifluoromethyl analogue that shows promise in research related to high-density lipoprotein (HDL) and low-density lipoprotein (LDL) with potential implications for coronary heart disease (CHD).

PCSK9 modulator-2 (Compound 1) 是一种有效的PCSK9调节剂（EC50 = 202 nM）， 具有用于高脂血症的研究潜力。PCSK9 是降低低密度脂蛋白胆固醇 (LDL-C) 的靶点。

PCSK9 modulator-3 (Compound 13) 是PCSK9的有效调节剂，EC50值为 2.46 nM，在高脂血症研究中具有潜力。PCSK9 是已证实的降低低密度脂蛋白胆固醇 (LDL-C) 的靶点。

PCSK9 modulator-4 (Compound 21) 是可以用于高血脂研究的，PCSK9的有效调节剂 (EC 50 = 0.15 nM)。PCSK9 是得到验证的一种降低低密度脂蛋白胆固醇 (LDL-C) 的靶标。

AMPK activator 6 (Compound GC) 可降低 HepG2 和 3T3-L1 细胞中的脂质含量并激活AMPK 通路。AMPK activator 6 对血清中甘油三酯 (TG)、总胆固醇 (TC)、低密度脂蛋白-C (LDL-C) 和其他生化指标的增加有显著的抑制作用。AMPK activator 6 在非酒精性脂肪肝（NAFLD）和代谢综合征中有研究价值。

Pitavastatin (NK-104) sodium 是一种有效的羟甲基戊二酰-CoA(HMG-CoA) 还原酶抑制剂，也是一种高效的肝细胞低密度脂蛋白胆固醇 (LDL-C) 受体诱导剂。Pitavastatin sodium 在 HepG2 细胞中，能够抑制乙酸合成胆固醇 (IC50: 5.8 nM) 。Pitavastatin sodium 表现出抗动脉粥样硬化、抗哮喘、抗骨关节炎、神经保护、抗肿瘤、肝保护和肾保护作用。

Bambuterol is a prodrug of β2-agonist commonly used for the treatment of asthma and chronic obstructive pulmonary disease (COPD) with the advantage of once daily dosing and favorable side effect profile. Administration of a single-dose of R-bambuterol resulted in dose-dependent reductions in the levels of plasma LDL-C, high-density lipoprotein cholesterol (HDL-C), total cholesterol (TC), apolipoprotein B (ApoB) and apolipoprotein A1 (ApoA1) at Tmax. R-bambuterol can lower the plasma levels of LDL-C, and marginally raise the ratio of ApoA1 ApoB (indicator of HDL-C LDL-C) with both a single dose and multiple doses. R-bambuterol was more potent in LDL-C lowering than rac-bambutero

6,8-Diprenyleriodictyol is an antioxidant, which inhibits Cu(2+)-mediated oxidation of human low density lipoprotein (LDL).

Azalanstat HCl is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat HCl has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg kg day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Azalanstat mesylate is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat mesylate has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes and hamster liver, by inhibiting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. When administered orally to hamsters fed regular chow, RS-21607 (50 mg kg day) lowered serum cholesterol in a dose-dependent manner (ED50 = 62 mg kg) in a period of 1 week. It preferentially lowered low density lipoprotein (LDL) cholesterol and apo B relative to high density lipoprotein (HDL) cholesterol and apo A-1.

Pitavastatin (NK-104) 是一种 3-羟基-3-甲基戊二酰辅酶A（HMG-CoA）还原酶抑制剂，具有降胆固醇和神经保护活性，抑制乙酸合成胆固醇，可减少氧化应激。Pitavastatin 是一种肝细胞低密度脂蛋白胆固醇 (LDL-C) 受体诱导剂，可用于研究冠状动脉粥样硬化、高胆固醇血症和急性冠脉综合征。Pitavastatin 结构不稳定，建议现用现配。

PCSK9-IN-13 是一种有效的PCSK9抑制剂， 可通过与 PCSK9 结合作用来拮抗低密度脂蛋白(LDL) 受体结合，其IC50值为 537 nM。

Milpocitide为针对低密度脂蛋白受体（human LDL receptor, LDLR）（293-333）的肽片段（EGF-like domain 1）的化合物。

N-Acetyldopamine dimer-2（compound 2）是一种从蝉皮黄色粉末中分离出来的N-acetyldopamine二聚体，具有抗氧化和抗炎作用。它能抑制氧化低密度脂蛋白（LDL）的氧化、ROS的生成、NO的生成以及NF-κB的活性。

Bococizumab(PF-04950615) 是一种针对PCSK9的人源化mAb，也是一种在肝脏中合成PCSK9的抑制剂，可降低低密度脂蛋白胆固醇 (LDL-C) 在血液中的含量。Bococizumab 可用于治疗高胆固醇血症。