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32

抑制剂 & 化合物

4

天然产物

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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。
T14667	BLT-1	Others; HCV Protease	Microbiology/Virology; Others; Proteases/Proteasome
	BLT-1 是一种氨基硫脲铜螯合剂，是一种选择性清除受体 B1 型 (SR-BI) 抑制剂，抑制高密度脂蛋白 (HDL) 和 SR-BI 介导的细胞之间的脂质转移。
T15549	Icosabutate	Others	Others
	Icosabutate is a structurally engineered and orally active ω-3 polyunsaturated fatty acid. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia.
T0841	Bezafibrate BM15075,苯扎贝特	PPAR	DNA Damage/DNA Repair; Metabolism
	Bezafibrate (BM15075) 是一种降血脂剂，是PPAR 的激动剂，对人以及鼠PPARα、PPARγ和PPARδ的EC50分别为 50、60和20 μM，以及 90、55 和110 μM。
T13601	CDD3506 1-TRITYL-1H-IMIDAZOL-4-AMINE	P450	Metabolism
	CDD3506 (1-TRITYL-1H-IMIDAZOL-4-AMINE) 能够诱导肝CYP3A 的活动，增强高密度脂蛋白胆固醇的水平。
T13600	CDD3505 4-nitro-1-trityl-1H-imidazole	P450	Metabolism
	CDD3505 (4-nitro-1-trityl-1H-imidazole) 能够诱导肝CYP3A 的活动，增强高密度脂蛋白胆固醇的水平。
T11386L	Gemcabene PD-72953	Others	Others
	Gemcabene (PD-72953) 是一种具有抗炎活性的降脂剂。 Gemcabene 降低低密度脂蛋白胆固醇和甘油三酯，提高高密度脂蛋白胆固醇，并降低促炎急性期蛋白、C 反应蛋白。
T1415	Gemfibrozil 吉非罗齐,CI-719,Jezil,Decrelip,Lopid	P450; Adrenergic Receptor; PPAR	DNA Damage/DNA Repair; GPCR/G Protein; Metabolism; Neuroscience
	Gemfibrozil (CI-719) 是一种PPAR-α激活剂，可作为降脂药。它也是P450非选择性抑制剂，对 CYP2C9、2C19、2C8 和 1A2 的Ki 值分别为 5.8、24、69 和 82 μM。
T36126	TMP-153
	Acyl-CoA:cholesterol acyltransferase (ACAT) catalyses the esterification of excess cellular cholesterol with fatty acids and is important for intestinal cholesterol absorption, hepatic lipoprotein secretion, and cholesterol accumulation in vascular tissues. ACAT inhibitors improve plasma lipid profile and ameliorate proteinuria in nephrotic animals. TMP-153 is a quinolyl derivative that inhibits ACAT with IC50 values of 5-10 nM in various animals. At 0.5-1.5 mg/kg, TMP-153 dose-dependently reduc...
T35603	Oleic Acid-2,6-diisopropylanilide
	AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of acylCoA:cholesterol acyltransferase with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide decreased low density lipoproteins and elevated high density lipoprotein levels when administered at 0.05%.
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).
T15004	CP-532623	CETP	Metabolism
	CP-532623, a close structural analog of Torcetrapib, is a CETP inhibitor with highly lipophilic properties. It elevates high-density lipoprotein cholesterol.
T2968L	Hyodeoxycholic acid sodium salt Sodium hyodeoxycholate,HDCA sodium
	Hyodeoxycholic acid sodium salt is a natural secondary bile acid. It improves high-density lipoprotein function, reduces farnesoid X receptor antagonist bile acids, and induces strong cytotoxicity, apoptosis, and IL-8 synthesis.
T68504	Obicetrapib calcium
	Obicetrapib calcium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
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).
T68505	Obicetrapib sodium
	Obicetrapib sodium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
T68503	Obicetrapib potassium
	Obicetrapib potassium is a cholesteryl ester transfer protein (CETP) inhibitor. CETP inhibitors substantially increase the concentration of high-density lipoprotein cholesterol (HDL-C), which may have a possible beneficial effect for cardiovascular disease risk reduction.
T64006	Lipid-lowering agent-1
	Lipid-lowering agent-1 是有效的降脂剂，能够明显抑制低密度脂蛋白胆固醇 (LDLC) 和促进高密度脂蛋白胆固醇 (HDLC) 产生的药理作用。Lipid-lowering agent-1 能够明显降低高脂饮食大鼠的脂肪。
T27228	E-3030 free acid E-3030,E3030,E 3030
	E-3030 free acid is a peroxisome proliferator-activated receptor (PPAR) agonist. E-3030 decreased blood glucose, triglyceride, non-esterified fatty acids, and insulin levels and increased blood adiponectin levels. Triglyceride- and non-high-density lipopr
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...
T36765	Palmitelaidic Acid methyl ester
	Palmitoleic acid is a common constituent of the triglycerides of human adipose tissue. Palmitoleic acid-based diets raise low-density lipoprotein cholesterol and diminish high-density lipoprotein cholesterol, even when dietary intake of cholesterol is maintained at a low level. Palmitelaidic acid is the trans isomer of the 16:1 fatty acid palmitoleic acid. While its effects on cholesterol levels are poorly studied, palmitelaidic acid can have very different effects from those of palmitoleic acid...
T75838	PDZ1 Domain inhibitor peptide TFA
	PDZ1 Domain inhibitor peptide TFA，一种环状肽，以 β-Ala 内酰胺侧链为接头，专一性靶向 PSD-95 的 PDZ1 域。此化合物能干扰 GluR6/PSD-95 间的相互作用，通过与 GluR6 的 C 末端竞争，抑制其在 PDZ1 域的结合。
T36234	5(Z),11(Z),14(Z)-Eicosatrienoic Acid
	5(Z),11(Z),14(Z)-Eicosatrienoic acid is a polyunsaturated fatty acid found in various natural sources including maritime pine (Pinus pinaster) seed oil (MPSO), gymnospermae leaves and seeds, and freshwater gastropods. A diet containing MPSO lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. 5(Z),11(Z),14(Z)-Eicosatrienoic acid methyl ester, when topically applied, reduces inflammatory processes, pot...
T79702	Nrf2 activator-9
	Nrf2 activator-9 (compound D-36) 是抑制oxLDL和HG诱导的HUVEC细胞凋亡的Nrf2激活剂，有助于预防动脉粥样硬化。该化合物可防止VEC损伤，展现出对心血管疾病的潜在治疗效果。
T35985	CAY10487
	The early stage of atherosclerosis is characterized by the aggregation of foam cells, so called a fatty streak, in the inner arterial wall. CAY10487 inhibits formation of fatty streak lesions of the thoracic aorta in high cholesterol-fed rabbits without affecting plasma lipid profiles or significantly inhibiting ACAT-1 or ACAT-2 activity. The percent area occupied by the atherosclerotic lesion in rabbits supplemented with 0.05% CAY10487 in the diet was 16.1% compared to 53.5% in control rabbits....
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...
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) ...
TP2176	amyloid A protein fragment [Homo sapiens]	Others	Others
	Amyloid A proteins (H2N-Ala-Gly-Leu-Pro-Glu-Lys-Tyr-OH) are a family of apolipoproteins associated with high-density lipoprotein in plasma. Different isoforms of SAA are expressed constitutively at different levels or in response to inflammatory stimuli.
T81900	LVGRQLEEFL (mouse) (TFA)
	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。
T81901	LVGRQLEEFL (mouse)
	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。
T35633	Pinolenic Acid ethyl ester
	Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an ...

化合物

Cat.No: T2499

Synonym: CP-529414,托彻普

Target: CETP

Cat.No: T14667

Target: Others, HCV Protease

Cat.No: T15549

Target: Others

Cat.No: T0841

Synonym: BM15075,苯扎贝特

Target: PPAR

Cat.No: T13601

Synonym: 1-TRITYL-1H-IMIDAZOL-4-AMINE

Target: P450

Cat.No: T13600

Synonym: 4-nitro-1-trityl-1H-imidazole

Target: P450

Cat.No: T11386L

Synonym: PD-72953

Target: Others

Cat.No: T1415

Synonym: 吉非罗齐,CI-719,Jezil,Decrelip,Lopid

Target: P450, Adrenergic Receptor, PPAR

Cat.No: T36126

Oleic Acid-2,6-diisopropylanilide

Cat.No: T35603

Gemcabene calcium

Cat.No: T11386

Synonym: PD-72953 calcium

Target: Others

Cat.No: T15004

Target: CETP

Hyodeoxycholic acid sodium salt

Cat.No: T2968L

Synonym: Sodium hyodeoxycholate,HDCA sodium

Obicetrapib calcium

Cat.No: T68504

Cat.No: T38908

Obicetrapib sodium

Cat.No: T68505

Obicetrapib potassium

Cat.No: T68503

Lipid-lowering agent-1

Cat.No: T64006

E-3030 free acid

Cat.No: T27228

Synonym: E-3030,E3030,E 3030

Cat.No: T70660

Azalanstat mesylate

Cat.No: T70661

Palmitelaidic Acid methyl ester

Cat.No: T36765

PDZ1 Domain inhibitor peptide TFA

Cat.No: T75838

5(Z),11(Z),14(Z)-Eicosatrienoic Acid

Cat.No: T36234

Nrf2 activator-9

Cat.No: T79702

Cat.No: T35985

Cat.No: T68695

Cat.No: T35813

amyloid A protein fragment [Homo sapiens]

Cat.No: TP2176

Target: Others

LVGRQLEEFL (mouse) (TFA)

Cat.No: T81900

LVGRQLEEFL (mouse)

Cat.No: T81901

Pinolenic Acid ethyl ester

Cat.No: T35633

Cat. No.	Product Name	Target	Signaling Pathways
T4775	Arachidic acid eicosanoic acid,Icosanoic Acid,花生酸	Others; Endogenous Metabolite	Metabolism; Others
	Arachidic acid (Icosanoic Acid) 是一种存在于所有哺乳动物细胞中的长链脂肪酸，通常酯化为膜磷脂，是人体组织中丰富的多不饱和脂肪酸之一。
T3S1513	(20R)-Protopanaxadiol Protopanaxadiol,20R-Protopanaxadiol,(20R)-原人参二醇,(20R)-Protopanaxdiol	Others; Antibacterial	Microbiology/Virology; Others
	(20R)-Protopanaxadiol ((20R)-Protopanaxdiol) 是黑参中20(R)-人参皂甙 Rg3的一种三萜皂苷代谢物。它抑制幽门螺杆菌的生长，有抗肿瘤活性和细胞毒性。
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).
T36563	(E)-Guggulsterone
	Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hy...

天然产物

Cat.No: T4775

Synonym: eicosanoic acid,Icosanoic Acid,花生酸

Target: Others, Endogenous Metabolite

(20R)-Protopanaxadiol

Cat.No: T3S1513

Synonym: Protopanaxadiol,20R-Protopanaxadiol,(20R)-原人参二醇,(20R)-Protopanaxdiol

Target: Others, Antibacterial

Stachybotramide

Cat.No: TN5057

Target: LDL

(E)-Guggulsterone

Cat.No: T36563

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