cholesterol synthesis

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。

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。

Lathosterol 是胆固醇样分子，其血清浓度是全身胆固醇合成的指标。

Azalanstat (RS 21607) 是一种可口服的选择性哺乳动物羊毛甾醇 14-α-脱甲基酶抑制剂，具有降胆固醇活性,通过抑制细胞色素 P450 酶羊毛甾醇 14 α-去甲基化酶来抑制 HepG2 细胞、人成纤维细胞、仓鼠肝细胞和仓鼠肝脏中的胆固醇合成。

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。

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。

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。

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。

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。

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。

Cholesteryl Hemisuccinate (Cholesterol hydrogen succinate) 是一种经常使用在极性溶液中具有高溶解度的胆固醇类似物 ，具有保肝、抗癌和抑制肿瘤生长的作用。Cholesteryl Hemisuccinate 抑制对乙酰氨基酚 的肝毒性，并防止 AAP 诱导的肝细胞凋亡 和坏死 。Cholesteryl Hemisuccinate 抑制 DNA 聚合酶 和 DNA 拓扑异构酶 ，从而抑制 DNA 复制和修复以及细胞分裂。

(ZE)-Farnesyl Pyrophosphate ammonium salt((ZE)-法尼基焦磷酸三铵盐)是(E,E)-Farnesyl Pyrophosphate ammonium salt的异构体。(E,E)-Farnesyl Pyrophosphate是甲羟戊酸 (MVA) 途径的关键代谢中间体和TRPM2的激动剂，并且参与胆固醇合成、泛醌合成、蛋白质法尼基化修饰等生理过程。

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。

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.

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。

7α-Hydroxy-4-cholesten-3-one 是一种可穿过血脑屏障的胆汁酸前体，可作为肝胆汁酸合成的指标。7α-Hydroxy-4-cholesten-3-one 是一种孕烷 X 受体 (PXR) 激动剂。7α-Hydroxy-4-cholesten-3-one 可用于研究与胆汁酸生物合成缺陷有关的疾病。

Mevalonic acid lithium salt (MVA lithium salt) 是甲羟戊酸途径的前体物质，是细胞生长的启动剂，是胆固醇合成的关键物质，可刺激外周血人淋巴细胞中的 DNA 合成、形态转化和细胞循环。

CAP2 (Cholesterol-amino-phosphate 2) hydrochloride 是一种胆固醇氨基磷酸盐 (CAP) 类脂质，主要用于制备脂质纳米颗粒 (LNP)，这些颗粒可用于传递mRNA及其他生物有效载荷。

DSP-0390 是一种口服的emopamil binding protein (EBP) 抑制剂。该化合物能高效抑制EBP酶，该酶为胆固醇生物合成中的关键后期步骤之一。通过抑制新生胆固醇合成，DSP-0390可针对增殖过快的GBM细胞更选择性地诱导细胞毒性。在人类GBM的异种移植模型中，DSP-0390显示出了显著的抗肿瘤活性。

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

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。

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 and structure-activity relationship study of cytotoxic germanicane- and lupane-type 3β-O-monodesmosidic saponins starting from betulinBioorg. Med. Chem.15(18)6144-6157(2007)

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(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]

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 inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)