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 inhibitscyclooxygenase-2(COX-2). Enflicoxib does not inhibit cyclooxygenase-1 (COX-1). E-6087 shows anti-inflammatory, analgesic and antipyretic activities in animal models[1]. |
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体内研究 (In Vivo) | 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[1]. 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[2].
Animal Model: | Male and female Wistar rats (250 g)[1] | 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. |
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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 |
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溶解性数据 | In Vitro: DMSO : 100 mg/mL(246.71 mM;ultrasonic and warming and heat to 60℃) 配制储备液 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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 |