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Search Results for " cholesterol biosynthesis "

24

抑制剂 & 化合物

12

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T14362	AY 9944	Others	Others
	AY 9944 是特异性的胆固醇生物合成抑制剂。它抑制 7- 脱氢胆固醇 Δ7- 还原酶 (IC50:13 nM)，导致胆固醇不足和 7DHC 积累。在高剂量下，它可在培养的胚胎中抑制固醇 Δ7-Δ8 异构酶，造成胆固醇 8-en-3β-ol 的积累。
T26296	Triparanol 曲帕拉醇,MER-29,NSC 65345,NSC-65345,NSC65345	Apoptosis; Hedgehog/Smoothened	Apoptosis; GPCR/G Protein; Stem Cells
	Triparanol (NSC-65345) 干扰 Hedgehog 信号分子的翻译后修饰以及其受体 PTCH1 的甾醇传感域，导致 Hedgehog 信号的下调。 Triparanol 抑制人类肿瘤生长，是一种具有高眼毒性的抗血脂剂。
T35973	Cholesterol-5α,6α-epoxide Epoxycholesterol,5α,6α-epoxy Cholestanol,NSC 18176	Others	Others
	Cholesterol-5α,6α-epoxide (Epoxycholesterol) 是胆固醇氧化产生的代谢产物。在应用他莫昔芬和 PBPE 后，5α,6α-环氧胆甾烷醇通过与 LXRβ 结合诱导三酰甘油生物合成。
T12092	Monacolin J Antibiotic MB 530A,Lovastatin diol lactone,辛伐他汀内酯二醇	HMG-CoA Reductase; Autophagy	Autophagy; Metabolism
	Monacolin J (Antibiotic MB 530A) 是一种胆固醇生物合成抑制剂，抑制 HMG-CoA 还原酶的活性。
T25285	Dalvastatin RG-12561,RG 12561,RG12561	HMG-CoA Reductase	Metabolism
	Dalvastatin (RG-12561) 是一种可口服的 HMG-CoA 还原酶和降胆固醇合成的抑制剂。Dalvastatin 竞争性地抑制大鼠肝脏HMG-CoA还原酶，IC50值为3.4 nmol / l。 Dalvastatin 在在大鼠实验中，抑制肝切片中的胆固醇生物合成，ED50值为0.9。
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。
T15184	E 2012 (E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亚苄基]哌啶-2-酮	Gamma-secretase	Neuroscience; Proteases/Proteasome; Stem Cells
	E 2012 是一种γ 分泌酶调节剂，不会影响 Notch 加工，在胆固醇生物合成的末步抑制 3β-羟基固醇 Δ24-还原酶。它能够减少淀粉样蛋白 β-42 减少阿兹海默氏病，并在大鼠多次重复给药后诱发白内障。
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。
T20999	1-(2,3-Dichlorphenyl)-piperazine 1-(2,3-二氯苯基)哌嗪,DCPP,1-(2,3-二氯苯基)哌嗪盐酸盐	Others	Others
	1-(2,3-Dichlorphenyl)-piperazine (DCPP) 是一种有效的 DHCR7 抑制剂。 DHCR7 是胆固醇生物合成中的一种酶。
T15710	Lapaquistat T-91485	Others	Others
	Lapaquistat is a cholesterol biosynthesis inhibitor and is the active metabolite of TAK-475. Lapaquistat can reduce statin-induced myotoxicity in lipid-lowering therapy.
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)
T35321	Zymostenol delta(8)-Cholestenol,5a-Cholest-8-en-3b-ol,Δ8-Cholesterol	Endogenous Metabolite; ROR	Metabolism
	Zymostenol (5a-Cholest-8-en-3b-ol) 是一种 RORγ 激动剂，EC50为1 μM。Zymostenol 是胆固醇生物合成的后期前体。
T35589	Geranyl pyrophosphate triammonium
	Geranyl pyrophosphate is an intermediate in the mevalonate pathway. It is formed from dimethylallyl pyrophosphate and isopentenyl pyrophosphate by geranyl pyrophosphate synthase. Geranyl pyrophosphate is used in the biosynthesis of farnesyl pyrophosphate , geranylgeranyl pyrophosphate , cholesterol, terpenes, and terpenoids.
T71133	Azacosterol hydrochloride
	Azacosterol is a diaza derivative of cholesterol which acts as a hypocholesteremic agent by blocking delta-24-reductase causing accumulation of desmosterol. Azacosterol acts as an inhibitor of 24-dehydrocholesterol reductase (24-DHCR), preventing the formation of cholesterol from desmosterol. Although it primarily acts to inhibit 24-DHCR, the drug also inhibits other steps in cholesterol biosynthesis. The antifertility effects of the drug in birds are mediated by inhibition of steroid hormone pr...
T37039	Betulinic Aldehyde oxime
	Betulinic aldehyde oxime is a pentacyclic triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin .1It is active againstE. aerogenes,E. coli,E. faecalis,P. aeruginosa,S. aureus, andC. albicans, as well asL. donovaniamastigotes, when used at a concentration of 50 μM.1,2Betulinic aldehyde oxime (50 μM) is cytotoxic to Huh7 hepatocellular carcinoma cells.2
T74147	Larsucosterol (trimethylamine)
	Larsucosterol (DUR-928) trimethylamine，一种胆固醇代谢物，有效的肝 X 受体 (LXR) 拮抗剂，同时作为内源性脂肪生成的调节剂。该化合物通过下调 mRNA 水平和抑制 SREBP-1 的激活，有效抑制胆固醇的生物合成。
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...
T68219	Peraclopone
	Peraclopone is a hypolidemic drug. It is an inhibitor of 7-Dehydrocholesterol reductase. Peraclopone potently inhibits the final step in cholesterol biosynthesis. Feeding this agent to rats leads to a rapid replacement of membrane cholesterol with its immediate precursor 7-dehydrocholesterol, and a dramatic reduction in plasma sterol concentration. Peraclopone caused a dose-dependent decrease in cholesterol and a concomitant accumulation of provitamin D3 (7-dehydrocholesterol) in the skin, which...
T36318	28-Acetylbetulin
	28-Acetylbetulin is a lupane triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin that has been found inM. chiapensisand has anti-inflammatory and anticancer activities.1,2It inhibits LPS-induced nitric oxide (NO) and prostaglandin E2production by 55.9 and 69.5%, respectively, in RAW 264.7 cells (IC50s = 4.7 and 1.7 μM, respectively).128-Acetylbetulin induces cytotoxicity in a variety of cancer cells, including A549, HT-29, and MCF-7 cells (IC50s = 14.37, 10.96, and 11.3...
T78081	Farnesyl Pyrophosphate ammonium Farnesyl diphosphate ammonium
	Farnesyl pyrophosphate ammonium salt为15碳类异戊二烯代谢中间体，源自MVA途径，兼具TRPM2激动剂功能，能够触发TRPM2通道开放并促进离子流入细胞。它亦是胆固醇合成、泛醌合成、蛋白质法尼基化修饰以及GGPP合成的关键底物。
T69244	Betulonaldehyde
	Betulonaldehyde is a pentacyclic triterpenoid and derivative of the cholesterol biosynthesis inhibitor betulin that has been found in Betula. It is active against P. falciparum (IC50 = 3.36 µg/ml) and cytotoxic to NCI H187 lung cancer cells and non-cancerous Vero cells (IC50s = 19.23 and 17.09 µg/ml, respectively). Topical application of betulonaldehyde (1 mg/ear) reduces ear edema induced by phorbol 12-myristate 13-acetate (TPA; Item No. 10008014) in mice. It has also been used a precursor in t...
T70856	3-Oxobetulin Acetate
	3-Oxobetulin acetate is a derivative of the cholesterol biosynthesis inhibitor betulin. It inhibits the growth of P388 murine lymphocytic leukemia cells (EC50 = 0.12 µg/ml), as well as human MCF-7 breast, SF-268 CNS, H460 lung, and KM20L2 colon cancer cells (GI50s = 8, 10.6, 5.2, and 12.7 µg/ml, respectively), but not BxPC-3 pancreas or DU145 prostate cancer cells (GI50s = >10 µg/ml for both). 3-Oxobetulin acetate inhibits replication of X4 tropic recombinant HIV (NL4.3-Ren) in MT-2 lymphoblasto...
T73755	Farnesyl pyrophosphate
	Farnesyl pyrophosphate (Farnesyl diphosphate) 是一种由15个碳原子组成的异戊二烯类化合物，作为甲羟戊酸 (MVA) 途径的关键代谢中间体。它充当TRPM2 (TRP Channel) 的激动剂，通过激活并打开TRPM2通道，促使离子流入细胞。此外，Farnesyl pyrophosphate 在胆固醇合成、泛醌合成、蛋白质法尼基化修饰以及香叶基-香叶基焦磷酸 (GGPP) 合成过程中扮演着至关重要的底物角色。
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

Cat.No: T14362

Target: Others

Cat.No: T26296

Synonym: 曲帕拉醇,MER-29,NSC 65345,NSC-65345,NSC65345

Target: Apoptosis, Hedgehog/Smoothened

Cholesterol-5α,6α-epoxide

Cat.No: T35973

Synonym: Epoxycholesterol,5α,6α-epoxy Cholestanol,NSC 18176

Target: Others

Cat.No: T12092

Synonym: Antibiotic MB 530A,Lovastatin diol lactone,辛伐他汀内酯二醇

Target: HMG-CoA Reductase, Autophagy

Cat.No: T25285

Synonym: RG-12561,RG 12561,RG12561

Target: HMG-CoA Reductase

Cat.No: T4039

Target: Others

Cat.No: T15184

Synonym: (E)-1-[(1S)-1-(4-氟苯基)乙基]-3-[3-甲氧基-4-(4-甲基-1H-咪唑-1-YL)亚苄基]哌啶-2-酮

Target: Gamma-secretase

Cat.No: T1676

Synonym: 罗伐他汀,ZD 4522,瑞舒伐他汀

Target: Potassium Channel, HMG-CoA Reductase, Autophagy

1-(2,3-Dichlorphenyl)-piperazine

Cat.No: T20999

Synonym: 1-(2,3-二氯苯基)哌嗪,DCPP,1-(2,3-二氯苯基)哌嗪盐酸盐

Target: Others

Cat.No: T15710

Synonym: T-91485

Target: Others

28-Deoxybetulin methyleneamine

Cat.No: T38088

Cat.No: T35321

Synonym: delta(8)-Cholestenol,5a-Cholest-8-en-3b-ol,Δ8-Cholesterol

Target: Endogenous Metabolite, ROR

Geranyl pyrophosphate triammonium

Cat.No: T35589

Azacosterol hydrochloride

Cat.No: T71133

Betulinic Aldehyde oxime

Cat.No: T37039

Larsucosterol (trimethylamine)

Cat.No: T74147

3-Acetyl Betulinaldehyde

Cat.No: T35686

Cat.No: T68219

28-Acetylbetulin

Cat.No: T36318

Farnesyl Pyrophosphate ammonium

Cat.No: T78081

Synonym: Farnesyl diphosphate ammonium

Betulonaldehyde

Cat.No: T69244

3-Oxobetulin Acetate

Cat.No: T70856

Farnesyl pyrophosphate

Cat.No: T73755

Nicotinamide-d4

Cat.No: T69395

Cat. No.	Product Name	Target	Signaling Pathways
TN1576	Diallyl disulfide	IL Receptor; NOS; NF-κB	Immunology/Inflammation; NF-κB
	Diallyl disulfide 能够抑制人角鲨烯单加氧酶，抑制角鲨烯环氧化的 IC50为 400 μM。它也具有抗肿瘤作用，同miR-200b 和miR-22联合使用可增强该作用。
TN6715	7-Ketocholesterol	Others	Others
	7-Ketocholesterol 是胆固醇的代谢物。
T19711	Desmosterol Desmesterol,24-Dehydrocholesterol	Endogenous Metabolite	Metabolism
	Desmosterol(24-Dehydrocholesterol) 是一种胆固醇生物合成中间体，抑制巨噬细胞炎症小体活化，防止血管炎症和动脉粥样硬化。
T4923	7-Dehydrocholesterol Provitamin D3,7-DHC,7-去氢胆固醇	Endogenous Metabolite	Metabolism
	7-Dehydrocholesterol (Provitamin D3) 是合成胆固醇和维生素 D3的前体。7-Dehydrocholesterol 下调培养的 Smith-Lemi-Opitz 综合征皮肤成纤维细胞中的胆固醇生物合成。
T1664	Meglutol Dicrotalic acid,3-Hydroxy-3-methylglutaric acid,美格鲁托	Endogenous Metabolite; HMG-CoA Reductase; Autophagy	Autophagy; Metabolism
	Meglutol (3-Hydroxy-3-methylglutaric acid) 是一种抗血脂剂，可降低胆固醇、甘油三酯、血清 β-脂蛋白和磷脂。它抑制胆固醇生物合成中的限速酶羟甲基戊二酰辅酶 A 还原酶的活性。
T4717	25-Hydroxycholesterol 25-羟基胆固醇,25-羟基胆甾醇	Others; Endogenous Metabolite; HMG-CoA Reductase	Metabolism; Others
	25-Hydroxycholesterol 是胆固醇的代谢产物，由巨噬细胞响应 Toll 样受体激活而分泌。它有效抑制 B 细胞产生 IgA，EC50约为 65 nM。
T41054	γ-Glutamyl-S-allylcysteine L-γ-Glutamyl-(S)-Allyl-Cysteine	Antioxidant	oxidation-reduction
	γ-Glutamyl-S-allylcysteine (L-γ-Glutamyl-(S)-Allyl-Cysteine) 是从Allium sativum L.中提取的γ-谷氨酰肽。γ-Glutamyl-S-allylcysteine 具有抗糖化和抗氧化活性，可抑制胆固醇的生物合成。
T73808	Zymosterol
	Zymosterol 是一种胆固醇Cholesterol 生物合成代谢物。Zymosterol 是胆固醇的前体，主要存在于质膜中。Zymosterol 在细胞内循环。
TN1655	Ganoderal A	Others	Others
	The oxygenated sterols( 26-oxygenosterols ganoderol A, ganoderol B, ganoderal A, and ganoderic acid Y) from G. lucidum can inhibit cholesterol biosynthesis via conversion of acetate or mevalonate as a precursor of cholesterol.
T83158	Agistatin D
	Agistatin D，一种从镰刀菌属分离得到的吡喃缩醛类化合物，具有抑制胆固醇生物合成(cholesterolbiosynthesis)的功能。
T83157	Agistatin E
	Agistatin E是镰刀菌属分离得到的一种吡喃缩醛类化合物，具有抑制胆固醇生物合成（cholesterolbiosynthesis）的功能。
TN1060	Ganoderol A 灵芝醇 A,灵芝醇A	Others	Others
	Ganoderol A has significant anti-inflammatory activity and protection against UVA damage. it has an inhibitory effect on angiotensin converting enzyme activity and cholesterol biosynthesis.

天然产物

Diallyl disulfide

Cat.No: TN1576

Target: IL Receptor, NOS, NF-κB

7-Ketocholesterol

Cat.No: TN6715

Target: Others

Cat.No: T19711

Synonym: Desmesterol,24-Dehydrocholesterol

Target: Endogenous Metabolite

7-Dehydrocholesterol

Cat.No: T4923

Synonym: Provitamin D3,7-DHC,7-去氢胆固醇

Target: Endogenous Metabolite

Cat.No: T1664

Synonym: Dicrotalic acid,3-Hydroxy-3-methylglutaric acid,美格鲁托

Target: Endogenous Metabolite, HMG-CoA Reductase, Autophagy

25-Hydroxycholesterol

Cat.No: T4717

Synonym: 25-羟基胆固醇,25-羟基胆甾醇

Target: Others, Endogenous Metabolite, HMG-CoA Reductase

γ-Glutamyl-S-allylcysteine

Cat.No: T41054

Synonym: L-γ-Glutamyl-(S)-Allyl-Cysteine

Target: Antioxidant

Cat.No: T73808

Cat.No: TN1655

Target: Others

Cat.No: T83158

Cat.No: T83157

Cat.No: TN1060

Synonym: 灵芝醇 A,灵芝醇A

Target: Others

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