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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T2499	Torcetrapib CP-529414,托彻普	CETP	Metabolism
	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。
T7832	Ibrolipim NO-1886	LPL Receptor	GPCR/G Protein
	Ibrolipim (NO-1886) 是口服具有活力的脂蛋白脂肪酶 (LPL) 激活剂。它能够降低血浆甘油三酸酯，增加高密度脂蛋白胆固醇水平，具有肾保护和降血脂的作用。
T1771	Ro 48-8071 fumarate	Others	Others
	Ro 48-8071 fumarate 是一种氧化鲨烯环化酶抑制剂(IC50:6.5 nM)。
T20887	Atorvastatin Sodium Lipitor	LDL; Aquaporin; HMG-CoA Reductase	Membrane transporter/Ion channel; Metabolism
	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。
T76739	Bococizumab RN316,PF-04950615	Others	Others
	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。
T70504	6,8-Diprenyleriodictyol
	6,8-Diprenyleriodictyol is an antioxidant, which inhibits Cu(2+)-mediated oxidation of human low density lipoprotein (LDL).
T11386	Gemcabene calcium PD-72953 calcium	Others	Others
	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).
T15561	Imanixil HOE-402(free base)	Others	Others
	Imanixil is an inducer of the LDL receptor (LDLR) and it is also a potent cholesterol-lowering compound. It also inhibits very low density-lipoprotein (VLDL) production and consequently decreases atherosclerosis development.
T38908	MK-8262
	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).
T73008	PCSK9-IN-13
	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。
T60646	PCSK9 modulator-3
	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。
T60541	PCSK9 modulator-2
	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。
T36171	KDdiA-PC
	Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were recently isolated and purified from oxLDL, and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. KDdiA-PC is one of the most potent CD36 ligands among the oxLDL species. KDdiA-PC confers CD-36 scavenger receptor binding affinity to LDL at a frequency of only two...
T60764	PCSK9 modulator-4
	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。
T77144	Recaticimab
	Recaticimab (SHR-1209) 是一种针对 PCSK9 的人源化单克隆抗体。该药物通过结合 PCSK9 并促进其降解，增加肝细胞表面的低密度脂蛋白 (LDL) 受体数量，从而有效降低血浆 LDL 水平，实现降低血脂的效果。Recaticimab 对于治疗高胆固醇血症显示出潜在价值。
T68695	(R)-Bambuterol
	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 LD...
T70660	Azalanstat HCl
	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 l...
T70661	Azalanstat mesylate
	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...
T75537	N-Acetyldopamine dimer-2
	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。
T79051	PCSK9-IN-15
	PCSK9-IN-15（化合物5）是一种高效PCSK9抑制剂，亲和力强（KD<200 nM）。该化合物与胆固醇代谢相关，可调控低密度脂蛋白胆固醇（LDL-C）水平，适用于研究降低胆固醇及血脂异常。
T74577	Milpocitide
	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。
T62380	20-HC-Me-Pyrrolidine
	20-HC-Me-Pyrrolidine 是一种有效的 Aster 蛋白抑制剂，对 Aster-A、Aster-B 和 Aster-C 具有抑制作用， IC50 分别为 0.11 μM、0.06 μM 和 0.71 μM。20-HC-Me-Pyrrolidine 阻止 Aster 蛋白结合和转移胆固醇，抑制低密度脂蛋白 (LDL) 胆固醇向内质网 (ER) 的移动。
T62598	Pitavastatin sodium
	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。
T62052	AMPK activator 6
	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。
T7072	Pitavastatin
	Pitavastatin (NK-104) 是有效的羟甲基戊二酰-CoA(HMG-CoA)还原酶抑制剂。Pitavastatin 抑制乙酸合成胆固醇，在 HepG2 细胞中的IC50为 5.8 nM。Pitavastatin 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 具有抗动脉粥样硬化、抗哮喘、抗骨关节炎、抗肿瘤、神经保护、肝保护和肾保护等作用。
T35813	CAY10592
	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) ...
T77123	Orticumab
	Orticumab (MLDL1278A) 为靶向氧化或丙二醛修饰的低密度脂蛋白(LDL)抗体，特异性抑制氧化低密度脂蛋白(oxLDL)。通过参与调节针对oxLDL的自身免疫反应，Orticumab能够改善动物模型中的动脉粥样硬化现象，并在银屑病改善研究中发挥作用。

化合物

Cat.No: T2499

Synonym: CP-529414,托彻普

Target: CETP

Cat.No: T7832

Synonym: NO-1886

Target: LPL Receptor

Ro 48-8071 fumarate

Cat.No: T1771

Target: Others

Atorvastatin Sodium

Cat.No: T20887

Synonym: Lipitor

Target: LDL, Aquaporin, HMG-CoA Reductase

Cat.No: T76739

Synonym: RN316,PF-04950615

Target: Others

6,8-Diprenyleriodictyol

Cat.No: T70504

Gemcabene calcium

Cat.No: T11386

Synonym: PD-72953 calcium

Target: Others

Cat.No: T15561

Synonym: HOE-402(free base)

Target: Others

Cat.No: T38908

Cat.No: T73008

PCSK9 modulator-3

Cat.No: T60646

PCSK9 modulator-2

Cat.No: T60541

Cat.No: T36171

PCSK9 modulator-4

Cat.No: T60764

Cat.No: T77144

Cat.No: T68695

Cat.No: T70660

Azalanstat mesylate

Cat.No: T70661

N-Acetyldopamine dimer-2

Cat.No: T75537

Cat.No: T79051

Cat.No: T74577

20-HC-Me-Pyrrolidine

Cat.No: T62380

Pitavastatin sodium

Cat.No: T62598

AMPK activator 6

Cat.No: T62052

Cat.No: T7072

Cat.No: T35813

Cat.No: T77123

Cat. No.	Product Name	Target	Signaling Pathways
TN5057	Stachybotramide	LDL	Metabolism
	Stachybotramide preferentially stimulate the plasma cholesteryl ester transfer protein (CETP)-mediated transfer of cholesteryl esters (CE) from high density lipoprotein (HDL) to both very low density lipoprotein (VLDL) and low density lipoprotein (LDL).

天然产物

Stachybotramide

Cat.No: TN5057

Target: LDL

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