Rosuvastatin is relatively hydrophilic and is highly selective for hepatic cells; its uptake is mediated by the liver-specific organic anion transporter OATP-C. Rosuvastatin is a high-affinity substrate for OATP-C with apparent association constant of 8.5 μM. Rosuvastatin inhibits cholesterol biosynthesis in rat liver isolated hepatocytes with IC50 of 1.12 nM. Rosuvastatin causes approximately 10 times greater increase of mRNA of LDL receptors than pravastatin. Rosuvastatin (100 μM) decreases the extent of U937 adhesion to TNF-α-stimulated HUVEC. Rosuvastatin inhibits the expressions of ICAM-1, MCP-1, IL-8, IL-6, and COX-2 mRNA and protein levels through inhibition of c-Jun N-terminal kinase and nuclear factor-kB in endothelial cells.

In vivo

Rosuvastatin is efficient on reducing plasma liquids. Rosuvastatin (3 mg/kg) daily administration for 14 days decreases plasma cholesterol levels by 26% in male beagle dogs with normal cholesterol levels. In cynomolgus monkeys, Rosuvastatin decreases plasma cholesterol levels by 22% Rosuvastatin (20 mg/kg/day) administration for 2 weeks, significantly reduces very low-density lipoproteins (VLDL) in diabetes mellitus rats induced by Streptozocin. Rosuvastatin shows antiatherothromhotic effects in vivo. Rosuvastatin (1.25 mg/kg) significantly inhibits thrombin-induced transmigration of monocvtes across mesenteric venules via inhibition of the endothelial cell surface expression of P-selectin, and increases the basal rate of nitric oxide in aortic segments by 2-fold times. Rosuvastatin (20 mg/kg) inhibits ROS production, normalizes NO-dependent endothelial function and reduces platelet activation in diabetic rats induced by Streptozocin. Rosuvastatin displays cardioprotective effects in vivo. Rosuvastatin (80 mg) is shows to decrease infarct size and improve cardiac mechanical function after ischemia/reperfusion in animal model. The cardioprotective properties of Rosuvastatin may be due to the improvement of coronary blood flow, decrease in resistance of coronary arteries mediated by enhanced eNOS expression, and the subsequent increase in the production of vascular endothelial NO. Rosuvastatin (2.0 mg/kg) attenuates left ventricular hypertrophy produced by transaortic constriction in mice through regulation of Racl protein and NADPH oxidase activities.
Cell Data

cell lines：HL-60, U937, and NB-4 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

规格

英文别名

calcium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethan-3-ylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate

规格或纯度

Moligand™, 10mM in DMSO

英文名称

Rosuvastatin (ZD4522) calcium

生化机理

瑞舒伐他汀钙片（ZD4522）是一种 HMG-CoA 还原酶竞争性抑制剂，在无细胞试验中的 IC50 值为 11 nM。

储存条件

-80℃储存

运输条件

特低温运输

作用类型

抑制剂

作用机制

HMG-CoA 还原酶抑制剂

名称和识别符

EC号

627-028-1

分子类型

小分子

Isomeric SMILES

CC(C1=NC(=NC(=C1/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.CC(C1=NC(=NC(=C1/C=C/[C@@H](O)C[C@@H](O)CC(=O)[O-])C2=CC=C(C=C2)F)N(S(=O)(=O)C)C)C.[Ca+2]

PubChem CID

5282455

分子量

500.57

技术文档

📋 安全数据表 (SDS)

全面的危险、操作、储存及法规合规文件。

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✅ 分析证书 (COA)

批次质量数据。输入批号以获取对应 COA。

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🔬 规格说明书

该级别的完整质量属性和验收标准。

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高级数据

化学和物理性质

溶解性

Solubility (25°C) In vitro Water: 5 mg/mL (38.11 mM); DMSO: Insoluble;

比旋光度

-8° (C=1,CHCl3)

熔点

160 °C

安全和危险性（GHS）

象形图

GHS08, GHS09

信号词

Danger

危险声明

H410: 对水生生物有剧毒并具有长期持续影响

H372: 通过长时间或反复暴露对器官造成损害

H360: 可能损害生育力或未出生的孩子

H350: 可能导致癌症

H370: 对器官造成损害

H362: 可能对母乳喂养的孩子造成伤害

预防措施声明

P273: 避免释放到环境中。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P321: 特殊处理（请参阅此标签上的...）。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。

P270: 使用本产品时，请勿进食、饮水或吸烟。

P391: 收集溢出物

P263: 避免在怀孕期间/哺乳期间接触。

P203: 使用前，获取、阅读并遵守所有安全说明。

P318: 如果暴露或担心，请就医。

P308+P316: 如果暴露或担心：立即寻求紧急医疗救助。

P319: 如果你感到不适，请寻求医疗帮助。

Merck Index

8270

质检证书（CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):

输入批号以搜索分析图谱:

技术文档和文章

他汀类抗高血脂抗癌药物

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抗癌抗高血脂药物治疗

Statins Antihyperlipidemics Anticancer Agents

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血脂异常的代谢机制、新兴干预靶点与药物研究进展

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siRNA 反义寡核苷酸动脉粥样硬化血脂异常低密度脂蛋白胆固醇 PCSK9 脂蛋白（a） APOC3 ANGPTL3 脂蛋白脂酶

Metabolic Mechanisms, Emerging Therapeutic Targets, and Advances in Drug Research for Dyslipidemia

目录：技术文章

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siRNA Lipoprotein(a) Antisense oligonucleotide atherosclerosis PCSK9 APOC3 ANGPTL3 dyslipidemia low-density lipoprotein cholesterol lipoprotein lipase

此产品的引用文献

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引用文献

1. Jie Yang, Xiuhua Pan, Jun Zhang, Siyu Ma, Jianeng Zhou, Zengguang Jia, Yawen Wei, Zengyi Liu, Ning Yang, Qi Shen. (2022) Reprogramming dysfunctional dendritic cells by a versatile metabolism nano-intervenor for enhancing cancer combinatorial immunotherapy. Nano Today, [10.1016/j.nantod.2022.101618]
2. Jie Yang, Zengguang Jia, Jun Zhang, Xiuhua Pan, Yawen Wei, Siyu Ma, Ning Yang, Zengyi Liu, Qi Shen. (2022) Metabolic Intervention Nanoparticles for Triple-Negative Breast Cancer Therapy via Overcoming FSP1-Mediated Ferroptosis Resistance. Advanced Healthcare Materials, 11 (13): (2102799). [PMID:35395704] [10.1002/adhm.202102799]
3. Xie Qiu-shi, Zhang Jia-xin, Liu Ming, Liu Pei-hua, Wang Zhong-jian, Zhu Liang, Jiang Ling, Jin Meng-meng, Liu Xiao-nan, Liu Li, Liu Xiao-dong. (2020) Short-chain fatty acids exert opposite effects on the expression and function of p-glycoprotein and breast cancer resistance protein in rat intestine. ACTA PHARMACOLOGICA SINICA, 42 (3): (470-481). [PMID:32555444] [10.1038/s41401-020-0402-x]
4. Kyeong-Ju Lee, Yoon-Mi Lee, Seong-Bin Yang, Jun-Hyuck Lee, Ha Rin Kim, Ji-Hong Lim, Jooho Park. (2024) A novel chemically engineered multifunctional statin conjugate as self-assembled nanoparticles inhibiting bile acid transporters. JOURNAL OF CONTROLLED RELEASE, [PMID:38971425] [10.1016/j.jconrel.2024.07.008]
5. Yuan-yuan Zhai, Qiang Wang, Qi-yao Nong, Mei-yu Gao, Ying Zhang, Qin-wen Xiao, Yuan Tian, Zun-jian Zhang, Feng-guo Xu, Pei Zhang. (2025) Pitavastatin overcomes multi-drug resistance in CRC and NSCLC by targeting the NRP1-ZFX axis. BIOCHEMICAL PHARMACOLOGY, [PMID:40684995] [10.1016/j.bcp.2025.117183]
6. Meng Yan, Yuan Zhong, Sheng Ni, Shirong Zhang, Yingying Jiang, Li Zhu, Kun Zhang, Kaiyong Cai, Kai Qu, Chuanwei Li, Wei Wu. (2025) CCR2-Engineered Macrophage Membrane-Coated Metal-Polyphenol Nanozyme to Enhance Antioxidation Activity for Inhibiting the Atherosclerotic Progression. Advanced Healthcare Materials, [PMID:40974123] [10.1002/adhm.202502151]
7. Hao Hao, Juntao Hu, Ziyu Kuai, Fengjie Hao, Wantong Jiang, Nana Ran, Yuting He, Yanping Zhang, Yibing Huang, Yanfei Qi, Quan Luo. (2024) Enzyme-mediated multifunctional self-healing lysozyme hydrogel for synergistic treatment of chronic diabetic wounds. INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES, [PMID:39437956] [10.1016/j.ijbiomac.2024.136719]
8. Kyeong-Ju Lee, Seong-Bin Yang, Jae-Hyeon Lee, Bison Seo, Hyung-Sik Won, Jooho Park. (2025) Preparation and Therapeutic Evaluation of Engineered Semaglutide and Statin–Lipid Conjugate-Based Nanoparticle. Pharmaceutics, 17 (4): (480). [PMID:40284475] [10.3390/pharmaceutics17040480]
9. Xuesheng Hu, Lu Han, Yiying Tan, Peitong Wu, Yajing Li, Wanjie Liu, Jiaming Shen, Yishan Li, Ming Yang, Chunnan Li, Jiaming Sun. (2026) A new lanostane-type triterpene with lipid-lowering activity from Ganoderma lucidum and an additional analogue. Frontiers in Chemistry, [PMID:41647298] [10.3389/fchem.2025.1726447]
10. Xianzheng Sang, Yichao Ye, Chengzi Yang, Xiaoxiang Hou, Yangu Guo, Hantong Shi, Chunhui Wang, Wen Chen, Danfeng Zhang, Lijun Hou. (2026) Microglia as a key mediator in rosuvastatin-associated cognitive impairment. NEUROTOXICOLOGY, [PMID:41690424] [10.1016/j.neuro.2026.103405]