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CAS:169590-41-4 Deracoxib 地拉考昔 药物分子开发
发布时间:2024-04-09     作者:kx   分享到:

中文名 地拉考昔

英文名 deracoxib

中文别名 4-(3-(二氟甲基)-5-(3-氟-4-甲氧基苯基)-1H-吡唑-1-基)苯磺酰胺

密度 1.5±0.1 g/cm3

沸点 575.5±60.0 °C at 760 mmHg

分子式 C17H14F3N3O3S

分子量 397.372

闪点 301.9±32.9 °C

精确质量 397.070801

PSA 95.59000

LogP 2.54

外观性状 粉末

蒸汽压 0.0±1.6 mmHg at 25°C

折射率 1.610

储存条件 -20℃

"Deracoxib, a selective cyclooxygenase-2 inhibitor, is a non-narcotic, non-steroidal anti-inflammatory drug (NSAID). 

IC50 Value: 70 to 150 uM(inhibition of 3 osteosarcoma cell lines) [1]

Target: COX

in vitro: Concentration of deracoxib required for 50% inhibition of cell viability (IC50) was reached in all 3 osteosarcoma cell lines and ranged from 70 to 150 microM, whereas the IC50 for piroxicam was only reached in the POS cell line at 500 microM. Neither deracoxib nor piroxicam induced sufficient toxicity in fibroblasts to reach an IC50. Exposure of osteosarcoma cells to cytotoxic concentrations of deracoxib and piroxicam did not result in DNA fragmentation [1]. Concomitant treatment of cells with piroxicam and deracoxib resulted in significant induction of apoptosis at lower concentrations and accumulation of cells in the G /G  phase. Significant cytotoxic effects exhibited by the combination of piroxicam and deracoxib against canine mammary carcinoma cells in vitro suggest an attractive approach for the treatment of canine mammary carcinoma [2].

in vivo: Perioperative administration of deracoxib to dogs at 1-2 mg/kg/day for 3 days significantly improves analgesia in the postoperative surgical period after soft tissue surgery [3]. Dogs were treated PO with deracoxib at a dosage of 3 mg/kg/d (1.36 mg/lb/d) as a single-agent treatment for TCC. Tumor response was assessed via radiography, abdominal ultrasonography, and ultrasonographic mapping of urinary bladder masses. Toxic effects of deracoxib administration in dogs were assessed through clinical observations and hematologic and biochemical analyses. 24 dogs for which tumor response was assessed, 4 (17%) had partial remission, 17 (71%) had stable disease, and 3 (13%) had progressive disease; initial response could not be assessed in 2 of 26 dogs. The median survival time was 323 days. Median time to progressive disease was 133 days. Renal, hepatic, and gastrointestinal abnormalities attributed to deracoxib administration were noted in 4% (1/26), 4% (1/26), and 19% (5/26) of dogs, respectively [4]."

CAS:169590-41-4	Deracoxib	    地拉考昔     药物分子开发

包装:100mg,500mg,1g,10g,100g以及kg级别等公斤级大包装

纯度:99%

配送:惯例下常温**

包装:袋装

厂家:西安齐岳生物科技有限公司

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