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羅非考昔,Rofecoxib
  • 羅非考昔,Rofecoxib

羅非考昔|T1185|TargetMol

價格 311 565 410
包裝 50mg 200mg 100mg
最小起訂量 1mg
發(fā)貨地 上海
更新日期 2024-09-23
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產(chǎn)品詳情

中文名稱:羅非考昔英文名稱:Rofecoxib
CAS:162011-90-7品牌: TargetMol
產(chǎn)地: 美國保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
純度規(guī)格: 99.94%產(chǎn)品類別: 抑制劑
貨號: T1185
2024-09-23 羅非考昔 Rofecoxib 50mg/311RMB;200mg/565RMB;100mg/410RMB 311 TargetMol 美國 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.94% 抑制劑

Product Introduction

Bioactivity

名稱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.
細胞實驗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)
激酶實驗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.
體外活性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]
體內(nèi)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]
存儲條件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)
關(guān)鍵字inhibit | MK 0966 | Cyclooxygenase | MK0966 | Inhibitor | MK966 | Rofecoxib | COX | MK-966
相關(guān)產(chǎn)品Ibuprofen | Paradol | Acetaminophen | Indomethacin sodium hydrate | Diclofenac sodium
相關(guān)庫抗癌上市藥物庫 | 抗癌活性化合物庫 | 抗衰老化合物庫 | FDA 上市藥物庫 | 藥物功能重定位化合物庫
關(guān)鍵字: MK 966|||羅非昔布|||MK-0966|||羅非考昔|TargetMol

公司簡介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起,為北美、歐洲和亞洲從事藥物研發(fā)和生物學研究的科學家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務。公司下設篩選事業(yè)部,化學事業(yè)部,生物事業(yè)部和新材料部。 從虛擬篩選到實體化合物分子供應;從商業(yè)化產(chǎn)品銷售到個性化定制合成;從對明確靶點的分子篩選到對明確分子的多靶點篩選,從高通量篩選到化學結(jié)構(gòu)優(yōu)化,我們都可以滿足您的科研用品及技術(shù)服務的需求。 經(jīng)過在中國市場五年的精心耕耘,我們已成為篩選化合物領域優(yōu)秀的供應商,為超過五百家學校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩
成立日期 2013-04-18 (12年) 注冊資本 566.2651萬人民幣
員工人數(shù) 100-500人 年營業(yè)額 ¥ 1億以上
主營行業(yè) 化學試劑,生物活性小分子 經(jīng)營模式 貿(mào)易,試劑,定制,服務
  • TargetMol中國(陶術(shù)生物)
VIP 12年
  • 公司成立:12年
  • 注冊資本:566.2651萬人民幣
  • 企業(yè)類型:有限責任公司(自然人投資或控股)
  • 主營產(chǎn)品:小分子抑制劑,藥物篩選化合物庫,天然產(chǎn)物,活性分子化合物等
  • 公司地址:上海市閘北區(qū)江場三路28號4樓
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