全国服务咨询热线：
18438616290
18438616290
产品分类
Product Category详细介绍
| 品牌 | absin | CAS | 162011-90-7 |
|---|---|---|---|
| 分子式 | C17H14O4S | 纯度 | ≥99% |
| 分子量 | 314.36 | 货号 | abs47027541 |
| 规格 | 25mg | 供货周期 | 现货 |
| 主要用途 | used for the treatment of osteoarthritis | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
Rofecoxib 162011-90-7
| 产品描述 | |
| 描述 | Rofecoxib is used for the treatment of osteoarthritis, rheumatoid arthritis, acute pain in adults, and primary dysmenorrhea, as well as acute treatment of migraine attacks with or without auras. Rofecoxib is a solid. This compound belongs to the stilbenes. These are organic compounds containing a 1,2-diphenylethylene moiety. Stilbenes (C6-C2-C6 ) are derived from the common phenylpropene (C6-C3) skeleton building block. The introduction of one or more hydroxyl groups to a phenyl ring lead to stilbenoids. Rofecoxib has a half-life of 17 hours and its mean oral bioavailability at therapeutically recommended doses of 125, 25, and 50 mg is approximately 93%. The proteins that rofecoxib target include elastin and prostaglandin G/H synthase 2. Cytochrome P450 1A2, Cytochrome P450 3A4, Cytochrome P450 2C9, Cytochrome P450 2C8, and Prostaglandin G/H synthase 1 are known to metabolize rofecoxib. On September 30, 2004, Merck voluntarily withdrew rofecoxib from the market because of concerns about increased risk of heart attack and stroke associated with long-term, high-dosage use. |
| 纯度 | ≥99% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | 罗非考昔；MK 966 |
| 外观 | 灰白色(淡黄色)结晶粉末 |
| 可溶性/溶解性 | DMSO : 59 mg/mL (187.7 mM) |
| 生物活性 | |
| 靶点 | COX-2 |
| In vitro(体外研究) | 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(体内研究) | 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. |
| 参考文献 | |
| 参考文献 |
|
| 研究领域 | |
| 研究领域 | Immunology CancerTumor biomarkers CancerTumor immunology Drug DiscoverySmall Molecule DrugLead Compound Discovery |
产品咨询
地址：上海市浦东新区新浩路58号申江科创园18栋
邮箱：lanwu@univ-bio.com
传真：