Enflicoxib E 6087,99.90%

产品编号:Bellancom-19384| CAS NO:251442-94-1| 分子式:C16H12F5N3O2S| 分子量:405.34

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-19384
2500.00 杭州 北京(现货)
Bellancom-19384
4000.00 杭州 北京(现货)
Bellancom-19384
8000.00 杭州 北京(现货)
Bellancom-19384
12800.00 杭州 北京(现货)

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Enflicoxib E 6087

产品介绍 Enflicoxib (E 6087) 是一种非甾体抗炎化合物,可选择性抑制环氧合酶 2 (COX-2)。Enflicoxib 不抑制环氧合酶-1 (COX-1)。E-6087 在动物模型中显示出抗炎、镇痛和解热活性。
生物活性

Enflicoxib (E 6087) is a nonsteroidal anti-inflammatory compound that selectively inhibits cyclooxygenase-2 (COX-2). Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models.

体外研究
体内研究

E-6132, one of Enflicoxib (E-6087) metabolites, also inhibits COX-2. After single oral administration of 5 mg/kg of E-6087 to rats, plasma concentrations of Enflicoxib at peak time are higher than those of E-6132, suggesting that activity is mainly due to Enflicoxib.
Enflicoxib (E-6087) is characterized by a long elimination half-life (20-35 h), a low plasma clearance (0.10-0.22 L/h/kg) and a relatively large volume of distribution (2-6 L/kg) in rats and dogs after single oral and intravenous doses. Enflicoxib and E-6132 (a pharmacologically active metabolite) show different pharmacokinetics. The higher percentage of Enflicoxib at early times suggests that Enflicoxib is the main compound responsible for in vivo activity, although E-6132 would contribute to the activity at later times.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female Wistar rats (250 g)
Dosage: 5 mg/kg
Administration: Administered by gastric gavage (10 mL/kg); a single oral dose
Result: Plasma concentrations of E-6087 at peak time are higher than those of E-6132.
体内研究

E-6132, one of Enflicoxib (E-6087) metabolites, also inhibits COX-2. After single oral administration of 5 mg/kg of E-6087 to rats, plasma concentrations of Enflicoxib at peak time are higher than those of E-6132, suggesting that activity is mainly due to Enflicoxib.
Enflicoxib (E-6087) is characterized by a long elimination half-life (20-35 h), a low plasma clearance (0.10-0.22 L/h/kg) and a relatively large volume of distribution (2-6 L/kg) in rats and dogs after single oral and intravenous doses. Enflicoxib and E-6132 (a pharmacologically active metabolite) show different pharmacokinetics. The higher percentage of Enflicoxib at early times suggests that Enflicoxib is the main compound responsible for in vivo activity, although E-6132 would contribute to the activity at later times.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male and female Wistar rats (250 g)
Dosage: 5 mg/kg
Administration: Administered by gastric gavage (10 mL/kg); a single oral dose
Result: Plasma concentrations of E-6087 at peak time are higher than those of E-6132.
性状Solid
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (246.71 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4671 mL 12.3353 mL 24.6706 mL
5 mM 0.4934 mL 2.4671 mL 4.9341 mL
10 mM 0.2467 mL 1.2335 mL 2.4671 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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