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19

抑制剂 & 化合物

15

天然产物

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Cat. No. Product Name Target Signaling Pathways
T17190 U18666A

Others; HCV Protease Microbiology/Virology; Others; Proteases/Proteasome
U18666A 是一种细胞渗透性药物,是一种胆固醇合成和转运抑制剂,抑制埃博拉病毒,登革热病毒和人类丙型肝炎病毒的复制。
T35371 Colesevelam Hydrochloride

Others Others
Colesevelam Hydrochloride 是一种胆汁酸隔离剂,在体外对甘胆酸均具有更高的亲和力。 Colesevelam Hydrochloride 抑制胆汁酸重吸收,导致胆汁酸合成增加并降低胆汁淤积性瘙痒症和克罗恩病患者的胆固醇水平。
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。
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。
T4317 PF 429242

NPC1L1; Lipid Membrane transporter/Ion channel; Metabolism
PF 429242 是甾醇调节元件结合蛋白 (SREBP) 位点 1 蛋白酶的竞争性抑制剂 (IC50 = 0.175 μM)。它对位点 1 蛋白酶对一组丝氨酸蛋白酶具有选择性。 PF-429242 抑制 CHO 细胞中胆固醇的合成速率 (IC50 = 0.53 μM)。
T26548 Acaterin

Acaterin, an inhibitor of acyl-CoA: cholesterol acyltransferase (ACAT), inhibits synthesis of cholesteryl ester in macrophage J774.
T40898 DMHCA

DMHCA, a potent, selective LXR agonist, specifically activates the LXR pathway's cholesterol efflux arm, avoiding triglyceride synthesis stimulation. This compound exhibits anti-inflammatory properties and is utilized in researching cholesterol homeostasis and diabetes.
T41015 Larsucosterol

DUR-928

Larsucosterol is a cholesterol metabolite from the nuclei of normal human liver tissues, epigenetically regulates the transcription of proteins and enzymes involved in lipid synthesis, inflammation, and apoptosis.
T38556 Larsucosterol sodium

DUR-928 sodium

Larsucosterol sodium is a cholesterol metabolite from the nuclei of normal human liver tissues, epigenetically regulates the transcription of proteins and enzymes involved in lipid synthesis, inflammation, and apoptosis.
T38088 28-Deoxybetulin methyleneamine

28-Deoxybetulin methyleneamine is a pentacyclic triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin .1It has been used in the synthesis of triterpene derivatives with antiviral activity. 1.Nitz, T.J., Montalbetti, C., Mears, R., et al.Extended Triterpene Derivatives(2008)
T71436 D561-0775

D561-0775 is a direct AMPK agonist, showing potential anti-cancer activity via inducing apoptosis, cell cycle arrest, suppressing glycolysis and cholesterol synthesis after activation of AMPK in gefitinib-resistant H1975 cells.
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...
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...
T13622 Cholestyramine

Colestyramine,考来烯胺,Cholestyramine resin

Others Others
Cholestyramine (Cholestyramine resin) 是一种胆汁酸结合树脂,能够抑制肠胆汁酸吸收导致增加粪便胆汁酸排泄,提高胆固醇胆汁酸合成。
T35686 3-Acetyl Betulinaldehyde

3-Acetyl betulinaldehyde is a triterpene and derivative of the cholesterol biosynthesis inhibitor betulin that has been found inA. japonica.1It is an intermediate in the synthesis of 3-acetylbetulinic acid, as well as various lupine and germanicane triterpenes and saponins with anticancer activity.2 1.Tung, N.H., Kwon, H.-J., Kim, J.-H., et al.An anti-influenza component of the bark of Alnus japonicaArch. Pharm. Res.33(3)363-367(2010) 2.Thibeault, D., Gauthier, C., Legault, J., et al.Synthesis a...
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。
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。
T36130 22(S)-hydroxy Cholesterol

22(S)-hydroxy Cholesterol,22β-hydroxy Cholesterol

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22...
T69395 Nicotinamide-d4

Nicotinamide-d4 is intended for use as an internal standard for the quantification of nicotinamide by GC- or LC-MS. Nicotinamide is an amide form of niacin, which is also known as vitamin B3, that can be biosynthesized in vivo or obtained through the diet. It is a precursor in the synthesis of the metabolic cofactor NAD+ and an inhibitor of sirtuin 1 (SIRT1; IC50 = <50 µM). Nicotinamide (10 µM) increases the activity of serine palmitoyltransferase (SPT) and the biosynthesis of ceramide, glucosyl...

化合物

U18666A
Cat.No: T17190
Synonym:
Target: Others, HCV Protease
Colesevelam Hydrochloride
Cat.No: T35371
Synonym:
Target: Others
Bococizumab
Cat.No: T76739
Synonym: RN316,PF-04950615
Target: Others
Gemfibrozil
Cat.No: T1415
Synonym: 吉非罗齐,CI-719,Jezil,Decrelip,Lopid
Target: P450, Adrenergic Receptor, PPAR
PF 429242
Cat.No: T4317
Synonym:
Target: NPC1L1, Lipid
Acaterin
Cat.No: T26548
Synonym:
Target:
DMHCA
Cat.No: T40898
Synonym:
Target:
Larsucosterol
Cat.No: T41015
Synonym: DUR-928
Target:
Larsucosterol sodium
Cat.No: T38556
Synonym: DUR-928 sodium
Target:
28-Deoxybetulin methyleneamine
Cat.No: T38088
Synonym:
Target:
D561-0775
Cat.No: T71436
Synonym:
Target:
Azalanstat mesylate
Cat.No: T70661
Synonym:
Target:
Azalanstat HCl
Cat.No: T70660
Synonym:
Target:
Cholestyramine
Cat.No: T13622
Synonym: Colestyramine,考来烯胺,Cholestyramine resin
Target: Others
3-Acetyl Betulinaldehyde
Cat.No: T35686
Synonym:
Target:
Pitavastatin sodium
Cat.No: T62598
Synonym:
Target:
Pitavastatin
Cat.No: T7072
Synonym:
Target:
22(S)-hydroxy Cholesterol
Cat.No: T36130
Synonym: 22(S)-hydroxy Cholesterol,22β-hydroxy Cholesterol
Target:
Nicotinamide-d4
Cat.No: T69395
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T0687 Simvastatin

辛伐他汀,MK-0733,MK 733

Apoptosis; Mitophagy; Ferroptosis; HMG-CoA Reductase; Autophagy Apoptosis; Autophagy; Metabolism
Simvastatin (MK 733) 是一种 HMG-CoA 还原酶抑制剂 (Ki=0.2 nM),具有口服活性。Simvastatin 具有降血脂活性,可以抑制肝脏产生胆固醇,还可以用于预防心血管疾病。
T4970 LANOSTEROL

羊毛甾醇,3β-Hydroxy-8,24-lanostadiene,8,24-Lanostadien-3β-ol

Endogenous Metabolite Metabolism
Lanosterol (3β-Hydroxy-8,24-lanostadiene) 是胆固醇合成的中间产物,能够诱导胆固醇合成的速率控制酶 HMG-CoA 还原酶的泛素化和降解。Lanosterol 可以抑制神经退行性疾病相关错误折叠蛋白的聚集和细胞毒性。
T15720 Lathosterol

Endogenous Metabolite Metabolism
Lathosterol 是胆固醇样分子,其血清浓度是全身胆固醇合成的指标。
T0760 Cholesterol

Cholesterin,Cholesteryl alcohol,胆固醇

Estrogen Receptor/ERR; MRP; Endogenous Metabolite; ROR Endocrinology/Hormones; Immunology/Inflammation; Metabolism
Cholesterol (Cholesteryl alcohol) 属于天然产物,是哺乳动物中的主要固醇,是一种雌激素相关受体 α (ERRα) 的激动剂。Cholesterol 广泛存在于动物的细胞膜,也是合成几种重要荷尔蒙及胆酸的材料。
TMA2440 Uridine 5'-monophosphate disodium salt

尿苷-5'-单磷酸二钠盐,Disodium UMP,尿苷酸二钠盐,Disodium uridine-5'-monophosphate,5'-UMP disodium salt,Disodium 5'-Uridylate

Others Others
Uridine 5'-monophosphate disodium salt (Disodium UMP) 是合成 RNA 的一种重要成分。
T5S0053 Coptisine

黄连碱,Coptisin

Indoleamine 2,3-Dioxygenase (IDO) Metabolism
Coptisine (Coptisin) 是一种从黄连中分离到的生物碱,是非竞争性的IDO 抑制剂,Ki=为 5.8 μM,IC50=6.3 μM。
T4749 Squalene

角鲨烯,Nikko Squalane EX,Super Squalene,AddaVax,all-trans-Squalene,trans-Squalene,Spinacene

Reactive Oxygen Species; Endogenous Metabolite; Antifungal Immunology/Inflammation; Metabolism; Microbiology/Virology; NF-κB
Squalene (AddaVax) 是胆固醇合成的中间产物,具有降血脂、保肝、心脏保护、抗氧化和抗毒活性等多种药理特性。它还具有抗真菌活性,可用于毛癣菌治疗的相关研究。
TCS2070 Homogentisic acid

高龙胆酸,2,5-dihydroxyphenylacetic acid,Homogentisinic Acid,Melanic acid

Antioxidant; Endogenous Metabolite Metabolism; oxidation-reduction
Homogentisic acid (2,5-dihydroxyphenylacetic acid) 是一种尿液和血清代谢物中的特定代谢物,可用于尿黑酸尿症的诊断。
T6480 D-Pantothenic acid

vitamin B5,pantothenate,D-泛酸

Others Others
D-Pantothenic acid (vitamin B5) 是必需的微量营养素,是辅酶 A 的前体,在很多生物过程中发挥关键作用,如调节碳水化合物,脂质,蛋白和核酸代谢。
T4947 3-Hydroxybutyric acid

Butanoic acid,3-羟基丁酸

Endogenous Metabolite Metabolism
3-Hydroxybutyric acid (Butanoic acid) 是一种人内源性代谢物,在 I 型糖尿病中升高。它能够调节膜脂的性质。
T83159 Agistatin B

Agistatin B是从真菌中分离出的霉菌毒素,能够抑制胆固醇合成(cholesterolsynthesis)。
TN1751 Hydroxycitric acid

ERK; p38 MAPK; Fatty Acid Synthase MAPK; Metabolism
(-)-Hydroxycitric acid (HCA) can inhibit fat synthesis and reduces food intake, the primary mechanism of action of HCA appears to be related to its ability to act as a competitive inhibitor of the enzyme ATP-citrate lyase, which catalyzes the conversion of citrate and coenzyme A to oxaloacetate and acetyl coenzyme A (acetyl-CoA), primary building blocks of fatty acid and cholesterol synthesis.
T10196 7α-Hydroxy-4-cholesten-3-one

Others Others
7α-Hydroxy-4-cholesten-3-one is an intermediate in the synthesis of bile acids from cholesterol. It is a PXR agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss and other diseases associated with defective bile acid biosynthesis.It is
T36226 Beauveriolide I

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific i...
T36227 Beauveriolide III

Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg/kg) reduces the size of aortic ...

天然产物

Simvastatin
Cat.No: T0687
Synonym: 辛伐他汀,MK-0733,MK 733
Target: Apoptosis, Mitophagy, Ferroptosis, HMG-CoA Reductase, Autophagy
LANOSTEROL
Cat.No: T4970
Synonym: 羊毛甾醇,3β-Hydroxy-8,24-lanostadiene,8,24-Lanostadien-3β-ol
Target: Endogenous Metabolite
Lathosterol
Cat.No: T15720
Synonym:
Target: Endogenous Metabolite
Cholesterol
Cat.No: T0760
Synonym: Cholesterin,Cholesteryl alcohol,胆固醇
Target: Estrogen Receptor/ERR, MRP, Endogenous Metabolite, ROR
Uridine 5'-monophosphate disodium salt
Cat.No: TMA2440
Synonym: 尿苷-5'-单磷酸二钠盐,Disodium UMP,尿苷酸二钠盐,Disodium uridine-5'-monophosphate,5'-UMP disodium salt,Disodium 5'-Uridylate
Target: Others
Coptisine
Cat.No: T5S0053
Synonym: 黄连碱,Coptisin
Target: Indoleamine 2,3-Dioxygenase (IDO)
Squalene
Cat.No: T4749
Synonym: 角鲨烯,Nikko Squalane EX,Super Squalene,AddaVax,all-trans-Squalene,trans-Squalene,Spinacene
Target: Reactive Oxygen Species, Endogenous Metabolite, Antifungal
Homogentisic acid
Cat.No: TCS2070
Synonym: 高龙胆酸,2,5-dihydroxyphenylacetic acid,Homogentisinic Acid,Melanic acid
Target: Antioxidant, Endogenous Metabolite
D-Pantothenic acid
Cat.No: T6480
Synonym: vitamin B5,pantothenate,D-泛酸
Target: Others
3-Hydroxybutyric acid
Cat.No: T4947
Synonym: Butanoic acid,3-羟基丁酸
Target: Endogenous Metabolite
Agistatin B
Cat.No: T83159
Synonym:
Target:
Hydroxycitric acid
Cat.No: TN1751
Synonym:
Target: ERK, p38 MAPK, Fatty Acid Synthase
7α-Hydroxy-4-cholesten-3-one
Cat.No: T10196
Synonym:
Target: Others
Beauveriolide I
Cat.No: T36226
Synonym:
Target:
Beauveriolide III
Cat.No: T36227
Synonym:
Target:
TargetMol Loading
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