罗非考昔|T1185|TargetMol

Rofecoxib
162011-90-7

￥311 50mg 起订

￥565 200mg 起订

￥410 100mg 起订

上海更新日期：2024-12-02

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产品详情:

中文名称：: 罗非考昔

英文名称：: Rofecoxib

CAS号：: 162011-90-7

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.94%

产品类别：: 抑制剂

货号：: T1185

Product Introduction

Bioactivity

名称	Rofecoxib
描述	Rofecoxib (MK 966) binds to and inhibits the enzyme cyclooxygenase-2 (COX-2), resulting in an inhibition of the conversion of arachidonic acid to prostaglandins. Rofecoxib is a synthetic, nonsteroidal derivative of phenyl-furanone with anti-inflammatory, antipyretic and analgesic properties and potential antineoplastic properties. COX-related metabolic pathways may represent key regulators of cell proliferation and neo-angiogenesis. Some epithelial tumor cell types overexpress pro-angiogenic COX-2.
细胞实验	The human osteosarcoma cell line has been shown to selectively express COX-2 by reverse transcription-polymerase chain reaction and immunoblot analysis, whereas undifferentiated human lymphoma U937 cells selectively express COX-1. The production of PGE2 by these cells after arachidonic acid challenge is used as an index of cellular COX-2 and COX-1 activity, respectively. Rofecoxib is preincubated for 5 to 15 minutes with the cells under serum-free conditions [Hanks' balanced salt solution (HBSS)] before a 10-minutes stimulation with 10 μM arachidonic acid and measurement of PGE2 production. COX activity in each cell line is defined as the difference in PGE2 concentrations in samples incubated in the presence or absence of arachidonic acid.(Only for Reference)
激酶实验	In vitro biochemical and pharmacological assaysinhibition studies with recombinant human COX-1 and COX-2: Microsomal preparations of recombinant human COX-1 and COX-2 are prepared from a vaccinia virus-COS-7 cell expression system. Recombinant human COX-1 and COX-2 are expressed in baculovirus-Sf9 cells, and enzymes are purified. Enzymatic activity is monitored continuously by either a fluorescence assay measuring the appearance of the oxidized form of the reducing agent cosubstrate homovanillic acid or by oxygen consumption. The HPLC assay for the assessment of inhibition of purified COX-1 by Rofecoxib with 0.1 μM arachidonic acid substrate concentration, the determination of the stoichiometry of the complex between COX-2 and Rofecoxib, the dissociation rate constant of the enzyme-inhibitor complex by recovery of enzymatic activity, and the recovery of intact Rofecoxib from that complex are all performed as described previously. The solvent system for the HPLC analysis of Rofecoxib is 15:85 MeOH/aqueous potassium phosphate (1 g/liter), with elution by a linear gradient of 15 to 75% MeOH over 25 minutes with detection at 275 nm on a Novapak C18 column.
体外活性	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. [1] 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. [2]
体内活性	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. [1] 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. [3]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 50 mg/mL (159.05 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字	inhibit \| MK 0966 \| Cyclooxygenase \| MK0966 \| Inhibitor \| MK966 \| Rofecoxib \| COX \| MK-966
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相关库	抗癌上市药物库 \| 抗癌活性化合物库 \| 抗衰老化合物库 \| FDA 上市药物库 \| 药物功能重定位化合物库

罗非昔布|||罗非考昔|||MK-0966|||MK 966|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

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