Ambeed 大中华区 CN | ZH

中文 - ZH English - EN

Ambeed.cn

搜索

关键字搜索批量搜索

首页 收藏 购物车0
首页 /
抑制剂/激动剂
药物研究 酶学
/
经典阳性药
酶抑制剂 代谢酶
/
HMGCR
心血管系统 单磷酸肌苷脱氢酶抑制剂
/ Rosuvastatin Calcium/瑞舒伐他汀钙

Rosuvastatin Calcium/瑞舒伐他汀钙 {[allProObj[0].p_purity_real_show]}

货号：A272688 同义名： Rosuvastatin hemicalcium; ZD 4522 Calcium

Rosuvastatin Calcium是一种竞争性合成HMG-CoA还原酶抑制剂，IC50值为11 nM。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Rosuvastatin Calcium/瑞舒伐他汀钙 化学结构 CAS号：147098-20-2
Rosuvastatin Calcium/瑞舒伐他汀钙 化学结构
CAS号：147098-20-2
Rosuvastatin Calcium/瑞舒伐他汀钙 3D分子结构
CAS号：147098-20-2
Rosuvastatin Calcium/瑞舒伐他汀钙 化学结构 CAS号：147098-20-2
Rosuvastatin Calcium/瑞舒伐他汀钙 3D分子结构 CAS号：147098-20-2
规格 价格 会员价 库存 数量
{[ item.pr_size ]} {[ size_append(item.pr_size_append, item.pr_am, item.pr_size) ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]}

{[ getRatePriceInt(item.pr_rmb, 1,1) ]}

{[ getRatePriceInt(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} 		{[ getRatePriceInt(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price, item.pr_am) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate,item.mem_isinteger) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate,item.mem_isinteger) ]} 现货 1周 咨询 - +
购物车0 收藏 询单

Rosuvastatin Calcium/瑞舒伐他汀钙 纯度/质量文件 产品仅供科研

货号：A272688 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
• Cell, 2025, 188, (21): 5847-5861.e11. Ambeed. [ A122167 ]
• Science, 2025, 387(6729): eadp5637. Ambeed. [ A875019 ]
• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025, 20, 1502-1513. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
更多 >

Rosuvastatin Calcium/瑞舒伐他汀钙 生物活性

描述 HMG-CoA reductase (HMGCR) catalyzes the rate-limiting step in cholesterol biosynthesis. Rosuvastatin calcium is a potent inhibitor of HMGCR with an Ki value of 0.1 nM and an IC50 value of 5.4 nM. The cholesterol synthesis in hepatocytes was inhibited by rosuvastatin calcium with an IC50 value of 0.2 nM. Rosuvastatin calcium also shows high affinity for liver-specific organic anio transport proteins (OATPs). The apparent Km value for the interaction between rosuvastatin calcium and OATP-C was 7.3 μM[3]. In papillary thyroid carcinoma B-CPAP cells, rosuvastatin calcium at 12.5 – 200 μM decreased cell viability with IC50 values of 12.9 μM and 4.6 μM for 48h- and 72h- incubations, respectively. Treatment with 50 μM rosuvastatin calcium for 48 hours led to G1 phase arrest in B-CPAP cells with a subG1 cell peak. Rosuvastatin calcium at 12.5 – 200 μM also caused a gradual decrease in the number of B-CPAP cells and an increase of the number of vacuoles at a dose-dependent manner. The caspase-3 activity and apoptotic rate in B-CPAP cells were significantly increased by rosuvastatin calcium at 12.5 μM[4]. Oral administration of rosuvastatin calcium in rats inhibited hepatic cholesterol synthesis with an ED50 of 0.8 mg/kg as measured 2 to 3 hours post treatment[3].
作用机制 Rosuvastatin calcium contains a dihydroxy heptenoic acid chain that mimics the HMG portion of HMGCR[3].

Rosuvastatin Calcium/瑞舒伐他汀钙 细胞实验

Cell Line
Concentration Treated Time Description References
THP-1 monocytes 10 µM 1 hour To investigate the effect of rosuvastatin on TNF-α-induced monocyte-endothelial cell adhesion. Results showed that rosuvastatin significantly inhibited TNF-α-induced adhesion of THP1 cells to HUVECs. Sci Rep. 2020 Apr 14;10(1):6383.
Human umbilical vein endothelial cells (HUVECs) 10 µM 1 hour To investigate the effect of rosuvastatin on TNF-α-induced monocyte-endothelial cell adhesion. Results showed that rosuvastatin significantly inhibited TNF-α-induced adhesion of THP1 cells to HUVECs and reduced the expression of ICAM and VCAM. Sci Rep. 2020 Apr 14;10(1):6383.
H9c2 cardiomyoblasts 20 µM 2 hours pretreatment followed by 12 hours stimulation Rosuvastatin inhibited TNF-α plus hypoxia-induced NLRP3 inflammasome activation and pyroptosis, as indicated by increased cell viability, decreased LDH release, and reduced PI uptake. Cell Death Dis. 2021 Jan 12;12(1):78.
RAW 264.7 macrophages 10 and 20 µM 24 hours To study the effect of Rosuvastatin on LPS-induced inflammatory response in RAW 264.7 macrophages in vitro. Results showed that Rosuvastatin significantly inhibited LPS-induced production of TNF-α and IL-6, and suppressed NF-κB activation. Aging (Albany NY). 2024 Jun 14;16(12):10424-10434.
RAW264.7 macrophages 5, 10, 25 µM 24 hours To evaluate the effect of rosuvastatin on ox-LDL-induced foam cell formation. Results showed that rosuvastatin significantly reduced lipid droplets deposition in RAW264.7 cells and attenuated foam cell formation. J Transl Med. 2021 Feb 10;19(1):62.
Human coronary artery smooth muscle cells (HCASMCs) 10 µM 24 hours To investigate the effect of rosuvastatin on TNF-α-induced migration and proliferation of smooth muscle cells. Results showed that rosuvastatin significantly inhibited TNF-α-induced migration and proliferation of HCASMCs and reduced the expression of Cyclin D1, Cyclin A2, PCNA, and c-Myc. Sci Rep. 2020 Apr 14;10(1):6383.
Human coronary artery endothelial cells (HCAECs) 0, 1, 2, 3 mg/ml 24, 48, 72 hours Rosuvastatin decreased apoptosis of HCAECs induced by CoCl2 by increasing anti-apoptosis Bcl-xl and Bcl-2 expression, and decreasing pro-apoptosis Bax, Bad, caspase-3 and caspase-9 expression. Mol Med Rep. 2020 Sep;22(3):2052-2062.
Rat nucleus pulposus cells 20 µM 72 hours Rosuvastatin promotes matrix anabolism and suppresses catabolism in response to TNF-α stimulation. Acta Biochim Biophys Sin (Shanghai). 2023 May 24;55(5):795-808.
Human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs) 0.3, 3, 30 µM approximately 4 minutes To evaluate the effect of rosuvastatin on cardiac action potential. Results showed that rosuvastatin significantly increased the maximum upstroke velocity (dV/dtmax) at 3 µM and 30 µM, and decreased the action potential duration (APD50) at 30 µM. Sci Rep. 2023 May 19;13(1):8108.

Rosuvastatin Calcium/瑞舒伐他汀钙 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
ApoE−/− mice High-fat diet-induced atherosclerosis model Oral 0.005% w/v Once daily for 13 weeks To investigate the preventive effect of rosuvastatin on periodontitis-induced atherosclerosis. Results showed that rosuvastatin significantly inhibited the development of periodontitis-induced atherosclerosis, reducing lipid deposition and atherogenic gene expression in the arterial wall and aortic sinus. Sci Rep. 2020 Apr 14;10(1):6383.
Adult male Wistar rats Acute model of hypertension Intravenous injection 0.5, 1, and 2 mg/kg 10 minutes apart, for 30 minutes Rosuvastatin enhanced the antihypertensive effect of cilostazol through effects on peripheral resistance, BRS, sympathovagal balance, endothelial dysfunction, and electrolytes balance. Naunyn Schmiedebergs Arch Pharmacol. 2024 Apr;397(4):2321-2334
SD rats Myocardial infarction model 1 mg/kg Once daily for 60 days Rosuvastatin treatment decreased mitochondrial reactive oxygen species, inflammation, mitochondrial damage, lipid catabolism, heart failure and myocardial infarction areas, while improving cardiac function indicators, right and left ventricular ejection fraction, and increasing expression levels of JAK and STAT3 in myocardial tissue. Mol Med Rep. 2020 Sep;22(3):2052-2062.
Kunming mice Intracerebral hemorrhage model Tail intravenous injection 1 mg/kg Starting at 6 hours post-surgery, once daily for 7 days To evaluate the therapeutic effects of nanomicelles in ICH mice, results showed that nanomicelles significantly reduced neuron degeneration, inhibited inflammatory cell infiltration, reduced brain edema, and improved neurological deficits. Int J Nanomedicine. 2021 Apr 20;16:2933-2947
Male Sprague-Dawley rats Adriamycin-induced myocardial injury model Gavage 1 mg/kg/day Once daily for 6 weeks To investigate the protective effects of rosuvastatin on adriamycin-induced myocardial injury. Results showed that rosuvastatin significantly reduced the levels of HMGB1 and RAGE in the myocardium and alleviated the inflammatory response. Int J Mol Med. 2018 Dec;42(6):3415-3423
ApoE−/− mice High-fat diet-induced atherosclerosis model Oral gavage 10 mg/kg/day Once daily for 20 weeks To evaluate the effect of rosuvastatin on atherosclerotic plaque burden. Results showed that rosuvastatin significantly reduced plaque areas in the aorta inner surface and the aortic sinus, improved lipid profiles, and reduced contents of inflammatory cytokines in the circulation. J Transl Med. 2021 Feb 10;19(1):62.
Sprague-Dawley rats Intervertebral disc degeneration model Intraperitoneal injection 10 mg/kg/day Once daily for 4 weeks Rosuvastatin inhibits IDD progression by alleviating pyroptosis and senescence and downregulating HMGB1 and p65. Acta Biochim Biophys Sin (Shanghai). 2023 May 24;55(5):795-808.
Sprague Dawley rats Azithromycin-induced cardiotoxicity model Intragastric tube administration 2 mg/kg/day Once daily for two weeks To evaluate the protective effect of Rosuvastatin against Azithromycin-induced cardiotoxicity. Results showed that Rosuvastatin significantly ameliorated ECG changes, biochemical and oxidative stress markers alterations, and restored the arrangement of cardiac muscle fibers. Life Sci. 2021 Mar 15;269:119099
Mice Paclitaxel-induced neuropathic pain model Intraperitoneal injection 3, 10, 30, 100 mg/kg Once daily for 7 consecutive days Rosuvastatin dose-dependently reduced mechanical allodynia and thermal hyperalgesia in paclitaxel-treated mice, showing a superadditive interaction when combined with duloxetine Int J Mol Sci. 2023 May 6;24(9):8359
Mice Paclitaxel-induced neuropathic pain model Intraperitoneal injection 3, 10, 30, 100 mg/kg Once daily for 7 consecutive days Rosuvastatin dose-dependently decreased mechanical allodynia and thermal hyperalgesia in paclitaxel-treated mice Int J Mol Sci. 2023 May 6;24(9):8359
C57BL/6 mice Coronary microembolization (CME) model Oral 40 mg/kg/day Once daily for three days before and three days after Rosuvastatin improved CME-induced cardiac contractile dysfunction, reduced myocardial fibrosis and microinfarct size, decreased serum LDH levels, and inhibited NLRP3 inflammasome activation and pyroptosis. Cell Death Dis. 2021 Jan 12;12(1):78.
C57BL/6 mice LPS-induced sepsis model Oral gavage 5 mg/kg/day Once daily for 20 weeks To investigate the protective effect of Rosuvastatin on LPS-induced sepsis in mice. Results showed that Rosuvastatin significantly reduced mortality, inhibited the production of inflammatory cytokines, and improved lung, liver, and kidney function. Aging (Albany NY). 2024 Jun 14;16(12):10424-10434.
Female Wistar rats High salt and cholesterol diet (HSCD)-induced cognitive impairment model Oral 5, 10, 15 mg/kg Once daily for 7 weeks To evaluate the effect of rosuvastatin in ameliorating HSCD-induced cognitive impairment via the Nrf2-ARE pathway. Results showed that rosuvastatin significantly reversed HSCD-induced changes in oxidative biomarkers, improved performance in neurobehavioral tests, and increased nuclear translocation of Nrf2. Redox Rep. 2018 Dec;23(1):168-179

Rosuvastatin Calcium/瑞舒伐他汀钙 动物研究

Dose Rat: 0.2 mg/kg - 20 mg/kg[3] (i.p.)
Administration i.p.

Rosuvastatin Calcium/瑞舒伐他汀钙 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01241903 Acute Coronary Syndrome ... 展开 >> Angioplasty, Transluminal, Percutaneous Coronary Hydroxymethylglutaryl-CoA Reductase Inhibitors Blood Platelets 收起 << Phase 1 Completed - United States, Kentucky ... 展开 >> University of Kentucky Dept of Cardiology Lexington, Kentucky, United States, 40536 收起 <<
NCT01241903 - Completed - -
NCT00747149 Type 2 Diabetes Phase 4 Completed - -

Rosuvastatin Calcium/瑞舒伐他汀钙 参考文献

[1]Schneck DW, Birmingham BK, et al. The effect of gemfibrozil on the pharmacokinetics of rosuvastatin. Clin Pharmacol Ther. 2004 May;75(5):455-63.

[2]Watanabe M, Koike H, et al. Synthesis and biological activity of methanesulfonamide pyrimidine- and N-methanesulfonylpyrrole-substituted 3,5-dihydroxy-6-heptenoates, a novel series of HMG-CoA reductase inhibitors. Bioorg Med Chem. 1997 Feb;5(2):437-44.

[3]Olsson AG, McTaggart F, Raza A. Rosuvastatin: a highly effective new HMG-CoA reductase inhibitor. Cardiovasc Drug Rev. 2002 Winter;20(4):303-28.

[4]Zeybek ND, Gulcelik NE, Kaymaz FF, Sarisozen C, Vural I, Bodur E, Canpinar H, Usman A, Asan E. Rosuvastatin induces apoptosis in cultured human papillary thyroid cancer cells. J Endocrinol. 2011 Jul;210(1):105-15.

Rosuvastatin Calcium/瑞舒伐他汀钙 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.00mL

0.20mL

0.10mL

4.99mL

1.00mL

0.50mL

9.99mL

2.00mL

1.00mL

Rosuvastatin Calcium/瑞舒伐他汀钙 技术信息

CAS号147098-20-2
分子式C44H54CaF2N6O12S2
分子量 1001.14
SMILES Code [O-]C(C[C@@H](C[C@@H](/C=C/C1=C(N=C(N=C1C2=CC=C(C=C2)F)N(S(=O)(C)=O)C)C(C)C)O)O)=O.[O-]C(C[C@@H](C[C@@H](/C=C/C3=C(N=C(N=C3C4=CC=C(C=C4)F)N(S(=O)(C)=O)C)C(C)C)O)O)=O.[Ca+2]
MDL No. MFCD04112702
别名 Rosuvastatin hemicalcium; ZD 4522 Calcium; ZD 4522; Rosuvastatin(calcium salt)
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, store in freezer, under -20°C
溶解方案

DMSO: 25 mg/mL(24.97 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 1 mg/mL(1 mM)，配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三

Tags: Rosuvastatin | 147098-20-2 | Rosuvastatin hemicalcium | ZD 4522 | ZD4522 | ZD-4522 | HMGCR Inhibitor | Metabolic Enzyme/Protease | Autophagy | Membrane Transporter/Ion Channel | Anti-infection | HMG-CoA Reductase (HMGCR) | Autophagy | Potassium Channel | Bacterial | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Rosuvastatin Calcium/瑞舒伐他汀钙 纯度/质量文件 | Rosuvastatin Calcium/瑞舒伐他汀钙 生物活性 | Rosuvastatin Calcium/瑞舒伐他汀钙 动物研究 | Rosuvastatin Calcium/瑞舒伐他汀钙 临床数据 | Rosuvastatin Calcium/瑞舒伐他汀钙 参考文献 | Rosuvastatin Calcium/瑞舒伐他汀钙 实验方案 | Rosuvastatin Calcium/瑞舒伐他汀钙 技术信息

AmBeed 相关网站 AmBeed.cn AmBeed.com
AmBeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
    • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    AmBeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质用途提供服务。

    尊敬的 AmBeed 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z