76
22
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T10063 |
LDL-IN-3
|
Antioxidant | oxidation-reduction |
LDL-IN-3 具有抗动脉粥样硬化和抗氧化活性。 | |||
T4039 |
BIBB 515
|
Others | Others |
BIBB 515 是口服具有活力的 2,3-氧化角鲨烯环化酶选择性抑制剂,在大鼠和小鼠中的 ED50值分别为 0.2-0.5 mg/kg 和 0.36-33.3 mg/kg (1-5 小时)。它主要利用抑制低密度脂蛋白的产生,从而发挥降脂作用。 | |||
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。 | |||
T9276 |
SBC-115337
|
Others; Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism; Others |
SBC-115337 是苯并呋喃化合物,也是 PCSK9抑制剂 (IC50:0.5 μM) 。 | |||
T2626 |
SBC-115076
SBC115076 |
Others; Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism; Others |
SBC-115076 是前蛋白转化酶枯草杆菌蛋白酶/ kexin 9型(PCSK9)抑制剂。其中PCSK9 是一种前蛋白转化酶,在 LDL 受体代谢中的重要物质。 | |||
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。 | |||
T6690 |
T0901317
N-(2,2,2-三氟乙基)-N-[4-[2,2,2-三氟-1-羟基-1-(三氟甲基)乙基]苯基]苯磺酰胺 |
Apoptosis; FXR; Liver X Receptor; ROR | Apoptosis; Metabolism |
T0901317 是一种口服有效且高度选择性的LXR 激动剂,对 LXRα 的EC50为 20 nM。它激活FXR,EC50为 5 μM。它是RORα和RORγ双重反向激动剂,Ki 值分别为 132 nM 和 51 nM。它诱导细胞凋亡,并抑制低密度脂蛋白受体缺失小鼠动脉粥样硬化的发展。 | |||
T4058 |
R-IMPP
|
Others; Serine/threonin kinase | Cell Cycle/Checkpoint; Metabolism; Others |
R-IMPP 是抗 PCSK9分泌的药物 (IC50=4.8 μM),靶向作用于 80S 核糖体,抑制 PCSK9 蛋白的翻译。 | |||
T9916 |
Alirocumab
|
Others | Others |
Alirocumab 是 PCSK9的人单克隆抗体。它能够特异性结合肝脏低密度脂蛋白 (LDL) 受体的下调剂 PCSK9,增强肝脏结合 LDL-胆固醇 (LDL-C) 的能力,降低血液中的 LDL-C 水平。它可用于研究高胆固醇血症。 | |||
T3625 |
Bempedoic acid
ETC1002,ESP-55016,ETC 1002,ETC-1002 |
ATP Citrate Lyase; AMPK | Chromatin/Epigenetic; Metabolism; PI3K/Akt/mTOR signaling |
Bempedoic acid (ETC1002) 是一种 ATP-柠檬酸裂解酶抑制剂,可激活AMPK。它是脂质和碳水化合物代谢的调节剂。 | |||
TP1881L1 |
Pep 2-8 ammonium salt(1541011-97-5 free base)
|
Others | Others |
Pep 2-8 ammonium salt(1541011-97-5 free base) 是 Proprotein 转化酶枯草杆菌蛋白酶/kexin 9 型 (PCSK9) 抑制剂。 PCSK9 与 LDL 受体结合的强效抑制剂 (IC50 = 0.8 μM)。恢复用 PCSK9 处理的 HepG2 细胞中的 LDL 摄取。 | |||
T1928 |
Anacetrapib
安塞曲匹,MK-0859 |
CETP | Metabolism |
Anacetrapib (MK-0859) 是 CETP 的抑制剂,能够抑制 rhCETP (IC50:7.9±2.5 nM) 和 C13S CETP 突变型 (IC50:11.8±1.9 nM) 的活性。 | |||
T4179 |
Probucol disuccinate
|
LDL | Metabolism |
Probucol disucinate 是一种 Probucol 的衍生物。其中 Probucol 是脂质调节的化合物,它能降低 LDL-cholesterol 水平。 | |||
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。 | |||
T67776 |
PCSK9-IN-11
|
Others | Others |
PCSK9-IN-11 (compound 5r) 是口服有效的 PCSK9 抑制剂。 PCSK9-IN-11 在 HepG2 细胞中抑制 PCSK9 转录活性 (IC50= 5.7 μM)。 PCSK9-IN-11 可以增加 LDL 受体 (LDLR) 蛋白水平,可用于动脉粥样硬化研究。 | |||
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。 | |||
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)。 | |||
T27832 |
Lifibrol
U 83860,K-12148,K-12.148,U-83860,K12148 |
Lipid | Metabolism |
Lifibrol (U-83860) 是一种胆固醇合成抑制剂。Lifibrol 具有抗胆固醇和降血脂的作用,可促进高胆固醇血症和混合型高脂血症患者体内低密度脂蛋白载脂蛋白 B-100 的转化。 | |||
T68042 |
CHF-4227
Chf4227,Chf 4227 |
Estrogen Receptor/ERR | Endocrinology/Hormones |
CHF-4227 是一种新型高效且具有选择性的雌激素受体调节剂,可降低胆固醇合低密度脂蛋白胆固醇浓度。 | |||
T38063 |
N-Acetyl lysyltyrosylcysteine amide
|
Glutathione Peroxidase | Metabolism |
N-Acetyl lysyltyrosylcysteine amide 是一种无毒的髓过氧化物酶 (MPO) 三肽抑制剂,具有有效性,可逆性和特异性。N-Acetyl lysyltyrosylcysteine amide 在体内可有效抑制 MPO 产生。N-Acetyl lysyltyrosylcysteine amide 减轻中风后大脑的神经元损伤,并保留脑组织和神经功能。N-Acetyl lysyltyrosylcysteine amide 抑制MPO依赖性次氯酸 (HOCl) 的生成,蛋白质硝化和 LDL 氧化。N-Acetyl lysyltyrosylcysteine amide 可用于研究支气管发育不良。 | |||
T0342 |
Carvedilol phosphate hemihydrate
Carvedilol phosphate,BM 14190 (phosphate hemihydrate),卡维地洛磷酸盐 |
VEGFR; Others; Potassium Channel; LDL; Integrin; Gap Junction Protein; NADPH; Adrenergic Receptor; Autophagy | Angiogenesis; Autophagy; Cytoskeletal Signaling; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Neuroscience; Others; Tyrosine Kinase/Adaptors |
Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) 是一种外消旋混合物,是一种非选择性β/α-1受体阻断剂,具有抗高血压活性且缺乏内在拟交感神经活性。 | |||
T5360 |
Eprotirome
伊罗替罗,KB2115 |
Thyroid hormone receptor(THR) | Endocrinology/Hormones |
Eprotirome (KB2115) 是一种肝脏选择性甲状腺激素受体 (thyroid hormone receptor, TR) 激动剂。它对 TRβ的亲和力略高于TRα。它降低了低密度脂蛋白 (LDL) 胆固醇的浓度,可用于研究血脂异常和肥胖症。 | |||
TP1111 |
Tirzepatide
LY-3298176 |
Glucagon Receptor | GPCR/G Protein |
Tirzepatide (LY-3298176) 是葡萄糖依赖性多肽 (GIP) 和胰高血糖素样肽-1 (GLP-1) 受体双重激动剂,具有神经保护活性,可改善血压并降低低密度脂蛋白 (LDL) 胆固醇和甘油三酯,可以用于研究糖尿病和肥胖症。 | |||
T70504 |
6,8-Diprenyleriodictyol
|
||
6,8-Diprenyleriodictyol is an antioxidant, which inhibits Cu(2+)-mediated oxidation of human low density lipoprotein (LDL). | |||
T30111 |
AR 12465
AR-12465 |
||
AR 12465 is a trapidil derivative which may affect LDL receptor mediated uptake and degradation of 125 I-LDL by human skin fibroblasts (HSF) and human hepatic cells (HEP G2). | |||
T76974 | Tafolecimab | ||
Tafolecimab (IBI-306) 是一种人源 lgG2 单克隆抗体,可特异性结合 PCSK-9并通过抑制 PCSK-9 介导的低密度脂蛋白受体的内吞作用降低 LDL-C 水平,进而增强对 LDL-C 的清除,导致 LDL-C 水平降低。Tafolecimab 可用于高胆固醇血症的研究。 | |||
T76377 |
Cdk2/Cyclin Inhibitory Peptide II
|
||
Cdk2/Cyclin Inhibitory Peptide II (Tat-LDL) 是一种 CDK2抑制剂,能以剂量依赖的方式杀死 U2OS 骨肉瘤细胞。 | |||
T74778 | ASM-IN-1 | Phospholipase | Metabolism |
ASM-IN-1是一种高效的口服活性ASM抑制剂,具有1.5 µM的IC50值。该化合物在减少主动脉弓及主动脉的脂质斑块方面表现出效果,并能够降低血浆中的神经酰胺以及Ox-LDL水平。ASM-IN-1展现了抗动脉粥样硬化与抗炎的活性。 | |||
TP1881 |
Pep2-8
Pep 2-8 |
||
Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. Potent inhibitor of PCSK9 binding to LDL receptor (IC50 = 0.8 μM). Restores LDL uptake in HepG2 cells treated with PCSK9. | |||
T35405 |
(±)9-HODE cholesteryl ester
|
||
(±)9-HODE cholesteryl ester was originally extracted from atherosclerotic lesions and shown to be produced by Cu2+-catalyzed oxidation of LDL. Later studies determined that 15-LO from rabbit reticulocytes and human monocytes were able to metabolize cholesteryl linoleate, a major component of LDL, to 9-HODE cholesteryl ester. | |||
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. | |||
T35404 |
(±)13-HODE cholesteryl ester
|
||
(±)13-HODE cholesteryl ester was originally extracted from atherosclerotic lesions and shown to be produced by Cu2+-catalyzed oxidation of LDL. Later studies determined that 15-LO from rabbit reticulocytes and human monocytes were able to metabolize cholesteryl linoleate, a major component of LDL, to 13-HODE cholesteryl ester. | |||
T28080 |
Mocravimod
KRP 203 free base,KRP-203,KRP203 |
||
Mocravimod is an agonist of sphingosine 1-phosphate receptor type 1. Mocravimod ameliorates atherosclerosis in LDL-R-/- mice. KRP-203 attenuates rat autoimmune myocarditis. KRP-203 combined with cyclosporine prolonged graft survival and abrogated transpla | |||
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... | |||
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。 | |||
T36727 |
9(S)-HODE
|
||
9(S)-HODE is produced by the lipoxygenation of linoleic acid in both plants and animals.[1],[2] It has been detected in atherosclerotic plaques, as an esterified component of membrane phospholipids and in oxidized LDL particles.[3] | |||
T77014 | Frovocimab | ||
Frovocimab (LY 3015014)为一种人源化IgG4单克隆抗体(mAb),其功能为中和PCSK9,通过抑制PCSK9与LDL受体(LDLR)的结合,促使已结合的PCSK9正常进行蛋白水解切割。 | |||
T79239 |
PCSK9-IN-19
|
||
PCSK9-IN-19 (Compound 1)作为一种PCSK9抑制剂,用于研究高LDL胆固醇水平及预防冠状动脉疾病。 | |||
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。 | |||
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。 | |||
T75778 |
COG 133 TFA
|
||
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。 | |||
T80658 |
Quercetin 7-glucuronide
Quercetin 7-O-β-glucuronide |
Drug Metabolite | Metabolism |
Quercetin 7-glucuronide(Quercetin 7-O-β-glucuronide),是 Quercetin 的一种代谢产物,从马达加斯加的 Uncarina 物种中可被分离提取。该化合物具有抑制 LDL 氧化的活性。 | |||
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... | |||
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). | |||
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... | |||
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). | |||
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。 | |||
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。 | |||
T78718 | Dim16 | ||
Dim16是一种同时抑制PCSK9和HMG-CoAR的化合物,其对PCSK9的IC50为19 nM,并且能够阻断PCSK9与LDLR的结合,此作用的IC50为0.8 nM。Dim16还能提升HepG2细胞对LDL的吸收。 | |||
T69408 | GW590735 sodium | ||
GW590735 is a potent and selective agonist of PPARα with an EC50 value of 4 nM for the expression a GAL4-responsive reporter gene and at least 500-fold selectivity versus PPARγ and PPARδ. GW590735 significantly increased HDL cholesterol, decreased LDL and VLDL cholesterol, and significantly reduced triglycerides. Maximal increases in HDL cholesterol were 37%, 53%, and 84% with fenofibrate, torcetrapib, and GW590735, respectively. |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T2S0265 |
Robinin
NSC 9222,刺槐素 |
TLR | Immunology/Inflammation |
Flavone glycoside from Robinia with antibacterial and diuretic properties; derived from kaempferol.The ability of robinin to reverse the multidrug resistance of the human colon cancer cell line Colo 320 expreβing MDR1/LRP was explored by monitoring their uptake of Rhodamine 123, but was shown to have minimal effect. Robinin (NSC-9222) was detected in lysates of the human breast cancer cell line MCF-7 using liquid chromatography-tandem maβ spectrometry. | |||
TN1438 |
beta-Amyrin acetate
beta-香树脂醇乙酸酯 |
Antioxidant; HMG-CoA Reductase; Epoxide Hydrolase; Antifungal | Metabolism; Microbiology/Virology; oxidation-reduction |
beta-Amyrin acetate 抑制 HMG-CoA 还原酶 (HMGCR) 和 sEH 活性,IC50 为 3.4 μM。 beta-Amyrin acetate 具有抗炎、抗真菌、抗氧化和抗高血脂活性。 | |||
T5214 |
Cholesteryl linoleate
CE(18:2(9Z,12Z)),Cholesterol Linoleate,Linoleic Acid cholesteryl ester,胆甾烯基亚油酸酯 |
Others; Endogenous Metabolite | Metabolism; Others |
Cholesteryl linoleate (Linoleic Acid cholesteryl ester) 是低密度脂蛋白和动脉粥样硬化病变中主要的胆固醇酯。它存在于 LDL 中的胆固醇酯,利用 LDL 受体相关蛋白转移到表达 15-脂氧合酶的巨噬细胞和 CHO 细胞的质膜,被氧化形成胆固醇亚油酸氢过氧化物。 | |||
T0254 |
Probucol
DH-581,普罗布考 |
Virus Protease; ABC; Lipid | Membrane transporter/Ion channel; Metabolism; Microbiology/Virology |
Probucol (DH-581) 是一种抗高脂血症药物,可通过增加 LDL 分解代谢率来降低血液中的胆固醇水平。 | |||
T2836 |
Isorhamnetin
3-methylquercetin,3'-Methylquercetin,Isorhamnetol,异鼠李素,3'-Methoxyquercetin |
MEK; PI3K; Endogenous Metabolite | MAPK; Metabolism; PI3K/Akt/mTOR signaling |
Isorhamnetin (3-methylquercetin) 是从中草药沙棘中提取的一种类黄酮,可通过抑制MEK1和PI3K 来抑制皮肤癌。 | |||
TN1511 |
Cleomiscosin A
|
LDL; Antioxidant; TNF | Apoptosis; Metabolism; oxidation-reduction |
Cleomiscosin A 来源于 Acer okamotoanum 的叶和树枝,对小鼠腹腔巨噬细胞的 TNF-α 分泌具有抑制活性。 Cleomiscosin A 可用于预防动脉粥样硬化病变中 LDL 氧化的研究。 | |||
TWO2727 |
Propane-1,2,3-triyl tripalmitate
Palmitic Triglyceride,Tripalmitin,Tripalmitoylglycerol,Glycerol Tripalmitate,三棕榈酸甘油酯 |
Others; Endogenous Metabolite | Metabolism; Others |
Propane-1,2,3-triyl tripalmitate (Glycerol Tripalmitate) 是内源性代谢产物的一种。 | |||
TN2967 |
Pinobanksin 3-acetate
3-O-Acetylpinobanksin |
Others; Antioxidant | Others; oxidation-reduction |
Pinobanksin 3-acetate (3-O-Acetylpinobanksin) 是一种短叶松素酯衍生物,是一种强抗氧化剂,存在于向日葵和蜂蜜中,可以抑制低密度脂蛋白的过氧化. | |||
T6S1930 |
Schisanhenol
五味子酚,Schizanhenol,Gomisin-K3 |
Antioxidant | oxidation-reduction |
Schisanhenol (Schizanhenol) 是一种UGT2B7的抑制剂,是一种天然化合物。 | |||
T4S2157 |
Campesterol
菜油甾醇,(24R)-5-Ergosten-3β-ol |
Endogenous Metabolite | Metabolism |
Campesterol ((24R)-5-Ergosten-3β-ol) 是一种植物甾醇,具有降胆固醇和抗癌的活性。 | |||
T3771 |
Methyl protodioscin
山药,Smilax saponin B,NSC-698790 |
Apoptosis | Apoptosis |
Methyl protodioscin (Smilax saponin B) 是一种甾二糖苷,能诱导细胞周期阻滞,具有抗肿瘤活性。 | |||
TN5171 |
Tricetin
|
Apoptosis; Others; Nrf2 | Apoptosis; Immunology/Inflammation; Others |
Tricetin 是一种从石榴中分离出的类黄酮。Tricetin 是 Keap1-Nrf2 蛋白相互作用(PPI)的强效竞争性抑制剂,通过激活 Nrf2/HO-1 信号通路和阻止线粒体依赖性细胞凋亡通路,保护帕金森病患免受 6-OHDA 诱导的神经毒性的影响。Tricetin 通过 Akt/GSK-1β途径抑制鼻咽癌的迁移和指示性蛋白酶早老素-1(PS-1)表达。Tricetin 抑制由Egr-1介导的氧化LDL 诱导的内皮炎症,保护大鼠软骨细胞免受IL-1β诱导的炎症和细胞凋亡。 | |||
T3427 |
Polydatin
Piceid,虎杖苷,Polydotin Peceid |
Apoptosis; Mitophagy; NF-κB; Autophagy | Apoptosis; Autophagy; NF-κB |
Polydatin (Piceid) 是从传统中药虎杖根中提取的一种天然产物,在多个实验模型中具有抗炎作用。它可抑制 G6PD,并诱导氧化和内质网应激。 | |||
T5S1172 |
Tiliroside
银椴甙,Tribuloside,银椴苷;椴树苷 |
Antioxidant | oxidation-reduction |
Tiliroside (Tribuloside) 是糖苷类黄酮,是 α-淀粉酶的非竞争性抑制剂(Ki:84.2 μM)。它抑制胃肠道中碳水化合物的消化和葡萄糖的吸收,具有抗糖尿病作用。 | |||
T2938 |
(E/Z)-Polydatin
云杉新甙,(E/Z)-虎杖苷,Polydatin,(E/Z)-Piceid |
Phospholipase | Metabolism |
(E/Z)-Polydatin (Polydatin) 是从虎杖的根和根茎中分离得到的一种单晶化合物。它具有抗血小板聚集、心脏保护作用、抗低密度脂蛋白 (LDL) 氧化作用、抗炎和免疫调节功能。 | |||
TN4956 |
Scandoside
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NF-κB; MAPK | MAPK; NF-κB |
Scandoside exerts anti-inflammatory effect via suppressing NF-κB and MAPK signaling pathways in LPS-induced RAW 264.7 macrophages.It also inhibits LDL-oxidation. | |||
TN1338 |
7Beta-Hydroxycholesterol
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LDL; Calcium Channel; MAPK | MAPK; Membrane transporter/Ion channel; Metabolism |
7beta-Hydroxycholesterol, a major cytotoxin in oxidized LDL, induces Ca(2+) oscillations, MAP kinase activation and apoptosis in human aortic smooth muscle cells. | |||
TN5057 |
Stachybotramide
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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). | |||
TN3675 | Cleomiscosin C | LDL | Metabolism |
Cleomiscosin C has antioxidant activity, it protects against the oxidative modification of apoB-100 induced by either Cu2+ or HOCl ( IC50s of 23.6 and 3.9 microM, respectively), suggests that it could be beneficial in preventing LDL oxidation in atheroscl | |||
T36560 |
(±)9-HpODE
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(±)9-HpODE is a racemic mixture of the fatty acid hydroperoxide product (9(S)-HpODE) formed from lipoxygenase action on linoleic acid. It shows antimicrobial activity against various fungal and bacterial pathogens and thus may play a role in plant defense. In mammalian species, monocyte-induced oxidization of LDL generates significant amounts of esterified 9-HpODE, which is rapidly reduced to 9-HODE. | |||
T83915 |
Norbixin hydrate
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Norbixin是一种在B. orellana中发现的类胡萝卜素,具有多样的生物活性。在无细胞测试中,它与过氧化物酶体增殖物激活受体γ (PPARγ)结合(Ki = 1.15 µM)。在心脑血管代谢综合征大鼠模型中,Norbixin (47.7 mg/kg) 能够减轻高血糖、高胰岛素血症和胰岛素抗性,降低血清脂质水平及心脏中硫代巴比妥酸反应性物质(TBARS)和谷胱甘肽(GSH)的水平。在胆固醇诱导的动脉粥样硬化兔模型中,它降低氧化型LDL和主动脉蛋白氧化水平,并减少动脉粥样硬化面积。Norbixin(每天0.1和1 mg/kg)减少汞诱导的大鼠肝细胞和白细胞DNA损伤。此外,它还能预防与年龄相关的黄斑变性(AMD)Abca4-/- Rdh8-/-小鼠模型中的光感受器退化。 | |||
T36749 |
Herboxidiene
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Herboxidiene is a polyketide originally isolated from S. chromofuscus that has diverse biological activities.[1],[2,][3],[4],[5] It inhibits growth of HeLa S3, SK-MEL-2, PC3, A549, and EBC-1 cells with GI50 values ranging from 7.4 to 62 nM.3 Herboxidiene is cytostatic against human umbilical vein endothelial cells (HUVECs; (IC50 = 26 nM)) and inhibits VEGF-induced invasion and tube formation of serum-starved HUVECs in a concentration-dependent manner, indicating antiangiogenic activity.[4] Herbo... |