SKF-86002 是一种具有口服活性的p38 MAPK抑制剂,具有抗炎、抗关节炎活性,可用于缓解疼痛的研究。SKF-86002 抑制脂多糖 (LPS) 刺激人单核细胞产生 IL-1 和 TNF-α (IC50= 1 μM)。SKF-86002 能抑制脂氧合酶和环氧合酶介导的花生四烯酸代谢。
生物活性 | SKF-86002 is an orally activep38 MAPKinhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipopolysaccharide (LPS)-stimulate human monocyteIL-1and TNF-α production (IC50= 1 μM). SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid[1][2][3]. |
体外研究 (In Vitro) | SKF-86002 (10 μM; 1 hour) inhibits apoptosis induced by stress stimulation with UV irradiation (UV)[1]. SKF-86002 does not inhibit UV-induced apoptosis in undifferentiated HL-60 cells[1]. SKF-86002 (10 μM; 72 hours) prevent IL-4-induced monocyte or U937 cell CD23 surface expression and protein formation with no effect on CD23 mRNA levels[4].
Western Blot Analysis[4] Cell Line: | U937 cells | Concentration: | 10 μM | Incubation Time: | 72 hours | Result: | Significantly reduced CD23 levels on IL-4-treated U937 cells. |
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体内研究 (In Vivo) | SKF-86002 (10-90 mg/kg; p.o.; daily; for 22 days) has antiarthritic activity[5].
Animal Model: | Lewis rats, with adjuvant-induced arthritis (AA)[5] | Dosage: | 10 mg/kg, 30 mg/kg, 90 mg/kg | Administration: | Oral administration, daily, for 22 days | Result: | Significantly decreased hindleg volumes after injection of adjuvant. |
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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 : 33.33 mg/mL(112.09 mM;Need ultrasonic) 配制储备液 1 mM | 3.3630 mL | 16.8152 mL | 33.6304 mL | 5 mM | 0.6726 mL | 3.3630 mL | 6.7261 mL | 10 mM | 0.3363 mL | 1.6815 mL | 3.3630 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.41 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (8.41 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.41 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
*以上所有助溶剂都可在本网站选购。 |