| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| R408064-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 环氧化酶-2 抑制剂 |
| 产品介绍 |
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. 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 lines：Jurkat CD4+ T cell leukemia cell line Concentrations：0.5 μM, 8 μM Incubation Time：15 minutes Powder Purity:≥99% |
| IC50 | COX-2, IC50: 18 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | C[S](=O)(=O)C1=CC=C(C=C1)C2=C(C(=O)OC2)C3=CC=CC=C3 |
| 分子量 | 314.36 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 20 mg/mL (60.16 mM); Water: Insoluble; Ethanol: Insoluble; |
|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Record the entire process by video | Conform |
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