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Firocoxib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Firocoxib图片
CAS NO:189954-96-9
包装:2mg, 5mg, 10mg, 50mg
包装与价格:
包装价格(元)
Free Sample (0.5-1 mg)电议
2mg电议
5mg电议
10mg电议
50mg电议

产品名称
ML 1785713
产品介绍

生物活性

Firocoxib is a coxib exhibiting high selectivity to inhibit COX-2. In vitro canine whole blood assays have demonstrated Firocoxib to be 350–430-fold more selective for COX-2 than for COX-1. COX-1 is constitutively expressed and enzymatically active in a variety of sites, including the stomach, intestine, kidneys, and platelets. COX-1 is the isoform largely responsible for the physiologic functions of eicosanoids, including gastric mucosal protection, renal blood flow, and vascular hemostasis. COX-2 expression is primarily induced by mediators such as serum growth factors, cytokines, and mitogens. COX-2 is primarily responsible for the synthesis of eicosanoids associated with inflammation.


化学数据

分子量336.4
分子式C17H20O5S
CAS号189954-96-9
纯度100.00%
溶解性(25°C)DMSO ≥ 45 mg/mL
储存和运输条件-20°C, sealed, protect from light
常温运输及临时存放

实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)

细胞实验
细胞系isolated peripheral blood mononuclear cells
方法Peripheral blood mononuclear cells were isolated by density gradient centrifugation and incubated at 37°C with medium alone, firocoxib (100 ng/mL), LPS (1 ng/mL or 1 μg/mL), or combinations of firocoxib and both LPS concentrations. After 4 hours, supernatants were collected and tested for prostaglandin E2 (PGE2) concentration with an enzyme inhibition assay, and gene expression in cell lysates was measured with PCR assays.
浓度100 ng/mL
处理时间4h

动物实验
动物模型Mouse Model of Incisional Pain by objective measurement of mechanical allodynia and thermal hyperalgesia using von Frey and Hargreaves equipment
配制diluted in sterile 0.9% physiologic saline
剂量10 or 20 mg/kg
给药处理intraperitoneally

不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)

小鼠大鼠豚鼠仓鼠
重量 (kg)0.020.151.80.40.0810
体表面积 (m2)0.0070.0250.150.050.020.5
Km系数36128520
动物 A (mg/kg) = 动物 B (mg/kg) × 动物 B的Km系数
动物 A的Km系数

例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。


储备液配制

以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。

Concentration / Solvent Volume / Mass1 mg5 mg10 mg
1 mM2.9727 mL14.8633 mL29.7265 mL
5 mM0.5945 mL2.9727 mL5.9453 mL
10 mM0.2973 mL1.4863 mL2.9727 mL