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| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
罗非昔布, 环氧化酶-2 抑制剂
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Rofecoxib 是一种COX-2抑制剂，IC50为18 nM。A selective Cox-2 inhibitor.
Information
Rofecoxib (MK-0966) is aCOX-2inhibitor withIC50of 18 nM.
In vitro
Rofecoxib inhibits the COX-2-dependent production of PGE2 in human osteosarcoma cells with an IC50 of 26 nM. Rofecoxib is a time-dependent inhibitor of purified human recombinant COX-2 with an IC50 of 0.34 μM. Rofecoxib causes inhibition of purified human COX-1 in a non-time-dependent manner. In a human whole blood assay, Rofecoxib selectively inhibits lipopolysaccharide-induced, COX-2-derived PGE2 synthesis with an IC50 value of 0.53 μM compared with an IC50 value of 18.8 μM for the inhibition of COX-1-derived thromboxane B2 synthesis after blood coagulation. Rofecoxib moderately inhibits phenacetin O-deethylation with an IC50 of 23 μM. And a 30-minute preincubation with microsomes and NADPH considerably increases the inhibitory effect of Rofecoxib with an IC50 of 4.2 μM. Inactivation of CYP1A2 by rofecoxib requires NADPH, and is characterized by a K i of 4.8 μM.
In vivo
Rofecoxib potently inhibits carrageenan-induced paw edema, carrageenan-induced paw hyperalgesia, lipopolysaccharide-induced pyresis with IC50 of 1.5 mg/kg, 1.0 mg/kg and 0.24 mg/kg, respectively. Rofecoxib also blocks adjuvant-induced arthritis with an IC50 of 0.74 mg/kg/day. Rofecoxib also has a protective effect on adjuvant-induced destruction of cartilage and bone structures in rats. Oral administration of rofecoxib decreases portal pressure in rats that are treated with CCl4 for 8 weeks. In addition, rofecoxib administration reduces the number of activated HSCs and to downregulate hepatic protein levels of three detected types of collagen, laminin, VEGF and CTGF in CCl4-treated rats.
Cell Data
cell lines：Jurkat CD4+ T cell leukemia cell line
Concentrations：0.5 μM, 8 μM
Incubation Time：15 minutes
Powder Purity:≥99%
规格
英文别名
MK-0966 | 4-(4-(methylsulfonyl)phenyl)-3-phenylfuran-2(5H)-one
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Rofecoxib
生化机理
罗非昔布（MK-0966）是一种 COX-2 抑制剂，IC50 为 18 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
环氧化酶-2 抑制剂
名称和识别符
EC号
803-260-0
分子类型
小分子
Isomeric SMILES
CS(=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3
PubChem CID
分子量
314.36
技术文档
高级数据
产品属性
| ALogP | 2.3 |
|---|
关联靶点（人）
MT-CO2
Tchem
细胞色素 c 氧化酶亚基 2(Cytochrome c oxidase subunit 2)
(1 活性数据)
PTGS2
Tclin
前列腺素 G/H 合酶 2(Prostaglandin G/H synthase 2)
(56 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 20 mg/mL (60.16 mM); Water: Insoluble; Ethanol: Insoluble;
熔点
209 °C
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H302: 吞食有害
预防措施声明
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P317: 如果被吞咽：请寻求医疗帮助。
WGK Germany
3
RTECS
LU5135000
Merck Index
8248
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
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）