57
10
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。 | |||
T1676 |
Rosuvastatin
罗伐他汀,ZD 4522,瑞舒伐他汀 |
Potassium Channel; HMG-CoA Reductase; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism |
Rosuvastatin (ZD 4522) 是一种抗血脂药,可竞争性抑制羟甲基戊二酰辅酶 A 还原酶,用于降低血浆胆固醇水平和预防心血管疾病。它降低低密度脂蛋白胆固醇、甘油三酯和 C-反应蛋白水平。它阻断人类醚-a-go-go 相关基因电流,IC50为 195 nM,延迟心脏复极化,延长动作电位持续时间和校正 QT 间期间隔。 | |||
T1510 |
Rosuvastatin calcium
ZD 4522 Calcium,ZD4522,Rosuvastatin hemicalcium,瑞舒伐他汀钙 |
Potassium Channel; HMG-CoA Reductase; Autophagy | Autophagy; Membrane transporter/Ion channel; Metabolism |
Rosuvastatin calcium (ZD4522) 是肝羟甲基戊二酰辅酶 A 还原酶的选择性和竞争性抑制剂,具有抗血脂活性。它降低成熟 hERG 的表达以及热休克蛋白 70 与 hERG 蛋白的相互作用,还降低低密度脂蛋白胆固醇、甘油三酯和 C-反应蛋白水平。它阻断人类醚-a-go-go 相关基因电流,延迟心脏复极化,来延长动作电位持续时间和校正 QT 间期间隔。 | |||
T25701 |
Levosemotiadil
SD 3212,SA 3212 |
LDL; Calcium Channel | Membrane transporter/Ion channel; Metabolism |
Levosemotiadil(SA 3212) 是一种新型钙拮抗剂,是一种非常有效的低密度脂蛋白氧化抑制剂。Levosemotiadil 可用于预防致死性心律失常。 | |||
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)。 | |||
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。 | |||
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。 | |||
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。 | |||
T6267 |
Lomitapide
AEGR-733,洛美他派,BMS-201038 |
CETP | Metabolism |
Lomitapide (AEGR-733) 是一种高效的微粒体甘油三酯转移蛋白(MTP)抑制剂,体内试验的IC50值为8 nM。 | |||
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。 | |||
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... | |||
T28009 |
ME-3221
ME3221 |
||
Apomine is an inhibitor of HMG-CoA-reductase. It promotes apoptosis of myeloma cells in vitro and is associated with a modulation of myeloma in vivo. Apomine enhances the antitumor effects of lovastatin on myeloma cells by down-regulating 3-hydroxy-3-meth | |||
T72025 |
PCSK9-IN-10
|
Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism |
PCSK9-IN-10 是一种有效的,具有口服活性的PCSK9抑制剂,IC50值为 6.4 µM。PCSK9-IN-10 增加LDLR 蛋白的表达并降低 PCSK9 的表达。PCSK9-IN-10 可减缓动脉粥样硬化进展。PCSK9-IN-10 具有研究高脂血症的潜力。 | |||
T2534 |
Pitavastatin calcium
P-872441,nisvastatin,itavastatin,Pitavastatin hemicalcium,匹伐他汀钙,NK-104 |
Apoptosis; Mitophagy; Endogenous Metabolite; HMG-CoA Reductase; Autophagy | Apoptosis; Autophagy; Metabolism |
Pitavastatin calcium (NK-104) 是一种羟甲基戊二酰-CoA 还原酶抑制剂。它在 HepG2 细胞中抑制乙酸合成胆固醇的IC50为 5.8 nM。它是高效的肝细胞低密度脂蛋白胆固醇受体诱导剂。具有抗癌活性。 | |||
T26644 |
Apomine
SK&F-99085,APB-231-A2,APB-231-A-2,SR-9223i,SK&F-99085,SR-45023A |
HMG-CoA Reductase | Metabolism |
Apomine (SR-9223i) 是一种 HMG-CoA-还原酶抑制剂,可在体外促进骨髓瘤细胞的凋亡,并与体内骨髓瘤的调节有关。 Apomine 加速 3-羟基-3-甲基戊二酰-CoA 还原酶的降解并刺激低密度脂蛋白受体活性。 Apomine 通过下调 3-羟基-3-甲基戊二酰-CoA 还原酶来增强洛伐他汀对骨髓瘤细胞的抗肿瘤作用。 | |||
T32892 |
LR 16
LR16,LR-16 |
||
LR 16 has potent effects on oxygen affinity of hemoglobin, on blood cholesterol and on low density lipoprotein. | |||
T70504 |
6,8-Diprenyleriodictyol
|
||
6,8-Diprenyleriodictyol is an antioxidant, which inhibits Cu(2+)-mediated oxidation of human low density lipoprotein (LDL). | |||
T70624 |
S 12340
|
||
S 12340 is a potent inhibitor of the oxidative modification of low-density lipoprotein. | |||
T22405 | Pravastatin | Others | Others |
Pravastatin is a lipoprotein-lowering drug via reversibly inhibiting hydroxymethylglutaryl-CoA (HMG-CoA) reductase and the synthesis of very-low-density lipoproteins. | |||
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). | |||
T15709 |
Lapaquistat acetate
TAK-475 |
Others | Others |
Lapaquistat acetate is a squalene synthase inhibitor. It also blocks the conversion of farnesyl diphosphate (FPP) to squalene. Lapaquistat acetate is used to Mevalonate Kinase Deficiency (MKD), it is effective at lowering low-density lipoprotein cholester | |||
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%. | |||
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... | |||
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。 | |||
T69477 | F81-1144b | ||
F81-1144b is a matrix metalloproteinase inhibitor which reduces secretion of very low density lipoprotein-triacylglycerol, thereby lowering TAG levels in serum and the liver. F81-1144b also lowers VLDL-TAG secretion, de novo FA synthesis in the liver, and serum levels of insulin and glucose. | |||
T36180 |
Azelaoyl PAF
|
||
Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which promote the differentiation of monocytes via the nuclear receptor PPARγ. One of these substances was recently isolated and purified from oxLDL, and identified as azelaoyl PAF. Azelaoyl PAF is a potent PPARγ agonist which competes for the thiazolidinedione binding site. Azelaoyl PAF is more potent than 15-deoxy-δ12,14-prostaglandin J2, and equipotent with rosiglitazone as a ligand for this receptor. | |||
T35956 |
PAz-PC
|
||
Oxidized low-density lipoprotein (oxLDL) particles contain low molecular weight species which are cytotoxic and pro-atherogenic. Many of these substances were isolated and purified from oxLDL and identified as phosphatidylcholine species containing a fragmented, oxidized short-chain fatty acid remnant at the sn-2 position. PAz-PC is one of the predominant oxLDL species and may be one of the important structural determinants of oxLDL. | |||
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... | |||
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。 | |||
T36549 |
CAY10486
|
||
Acyl-Coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis. CAY10486 inhibits human ACAT-1 and ACAT-2 equally with an IC50 value of approximately 60 μM. It also inhibits copper-mediated oxidation of low density lipoproteins by about 28% at a concentration of 3 μM. | |||
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。 | |||
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。 | |||
T14931 | Cerivastatin | Others | Others |
Cerivastatin is a highly potent, well-tolerated, and orally active HMG-CoA reductase inhibitor (Ki: 1.3 nM/L). Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition with anti-cancer effect. Cerivastatin r | |||
T32171 |
Iodoalphionic acid
NSC 11854,NSC-11854,Pheniodolum,NSC11854,Tenamid |
||
Iodoalphionic acid is the contrast medium for gallbladder examination. It is rarely found in the colon and can rarely masked the gallbladder. The density of the shadow from Iodoalphionic acid was greater than that produced by iodophthalein. It was reliabl | |||
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。 | |||
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。 | |||
T35984 |
CAY10485
|
||
Acyl-coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis. CAY10485 inhibits human ACAT-1 and ACAT-2 with an IC50 values of 95 and 81 μM, respectively. It also inhibits copper-mediated oxidation of low density lipoproteins by 91% at a concentration of 2 μM. | |||
T35580 |
POV-PC
|
||
Oxidized low-density lipoprotien (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. 1-(Palmitoyl)-2-(5-oxovaleroyl)-phosphatidylcholine, or POV-PC, is one of the oxLDL species derived from 2-arachidonoyl or eicosapentanoyl phospholipids. POV-PC conf... | |||
T36567 |
DPPP
|
||
DPPP is a probe that reacts stoichiometrically with hydroperoxides to yield the fluorescent molecule diphenyl-1-pyrenylphosphine oxide (DPPP-O). Plasma levels of lipid hydroperoxides of phosphatidylcholine, phosphatidylethanolamine, triglycerides, and cholesteryl esters have been measured by HPLC with a post column detection system using DPPP. DPPP has also been used as a fluorescent probe for the detection of low density lipoprotein and cellular oxidation. Fluorescence of DPPP-O can be monitor ... | |||
T36172 |
KOdiA-PC
|
||
Oxidized low-density lipoprotien (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. 1-(Palmitoyl)-2-(5-keto-6-octene-dioyl) phosphatidylcholine, or KOdiA-PC, is one of the most potent CD36 ligands among the oxLDL species. KOdiA-PC confers CD36 scave... | |||
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。 | |||
T70660 |
Azalanstat HCl
|
||
Azalanstat is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat 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 densi... | |||
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。 | |||
T70661 |
Azalanstat mesylate
|
||
Azalanstat is an anti-obesity drug acting as a lanosterol 14α-demethylase inhibitor. Azalanstat 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 densi... | |||
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。 | |||
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。 | |||
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。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T5S0246 |
Pseudoprotodioscin
山药 |
Others; Fatty Acid Synthase | Metabolism; Others |
Pseudoprotodioscin 是一种呋喃葡糖苷,抑制SREBP1/2和microRNA 33a/b 水平,降低胆固醇和甘油三酯合成相关的基因表达。 | |||
T5242 |
Triarachidin
Triarachin,1,2,3-Trieicosanoyl Glycerol,Glycerol Trieicosanoate,三花生精 |
Others; Endogenous Metabolite | Metabolism; Others |
Triarachidin (1,2,3-Trieicosanoyl Glycerol) 是内源性代谢产物的一种。 | |||
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。 | |||
T5280 |
3-Chloro-L-Tyrosine
3-氯-L-酪氨酸,3-Chlorotyrosine,Chlorotyrosine |
Others; Endogenous Metabolite | Metabolism; Others |
3-Chloro-L-Tyrosine (Chlorotyrosine) 是一种髓过氧化物酶催化氧化的特异性标志物,在从人动脉粥样硬化内膜分离的低密度脂蛋白中显著升高。 | |||
T4S0145 |
Corylifol A
Corylinin,补骨脂异黄酮A |
hCE; STAT; UGT | JAK/STAT signaling; Metabolism; Stem Cells |
Corylifol A (Corylinin) 是补骨脂中的一种天然产物,可抑制IL-6 诱导的STAT3激活和磷酸化,IC50值为0.81 μM。 | |||
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). | |||
TN4600 |
Myrianthic acid
|
PAFR; AChR | GPCR/G Protein; Neuroscience |
Myrianthic acid shows anticancer activity, it shows inhibitory activities on foam cell formation in human monocyte-derived macrophages induced by acetylated low-density lipoproteins at a 50 uM concentration. Myrianthic acid is equivalently inhibitive as acetylsalicylic acid (IC50: 57.0 microM) on epinephrine induced platelet aggregation. | |||
T77289 | 5-O-Methylembelin | ||
5-O-Methylembelin 是一种天然异香豆素,可抑制PCSK9、低密度脂蛋白受体 (IDOL) 和甾醇调节元件结合蛋白 2 (SREBP2) mRNA 的表达。 | |||
TN5174 | Trichosanatine | MMP; LDL; p38 MAPK; Lipoxygenase; ROS | Immunology/Inflammation; MAPK; Metabolism; Proteases/Proteasome |
Trichosanatine and squamosamide, as potential candidates as lead compounds for further study in drug development process with the PP2A- α protein. Trichosanatine can alleviate oxidized low-density lipoprotein induced endothelial cells injury via inhibiting the LOX-1/p38 MAPK pathway. | |||
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... |