Imrecoxib(BAP-909)艾瑞昔布是选择性环氧合酶 2 (COX-2) 抑制剂,IC50值为 18 nM,也可以抑制 COX1 活性,IC50值为 115 nM。Imrecoxib(BAP-909) 艾瑞昔布具有抗炎作用。
生物活性 | Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with anIC50value of 18 nM, it also inhibits COX1- activity with anIC50value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect[1]. |
IC50& Target[1] | Human COX-1 115 nM (IC50) | Human COX-2 18 nM (IC50) |
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体外研究 (In Vitro) | Imrecoxib (BAP-909) (0.1-10 μM; 24 hours) decreases COX-2 mRNA level induced by PMA+LPS at a dose dependent manner in U937 cells[1].
RT-PCR[1] Cell Line: | U937 cells | Concentration: | 0.1 μM; 1 μM; 10 μM | Incubation Time: | 24 hours | Result: | Decreased COX-2 mRNA level. |
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体内研究 (In Vivo) | Imrecoxib (BAP-909) (gastrointestinal administration; 5-20 mg/kg; 1 hour before carrageenan injection) inhibits carrageenan-induced acute inflammation, and the inhibitory effect is maximal at 4 hours[1].Imrecoxib (BAP-909) (gastrointestinal administration; 5-20 mg/kg; started on day 7; 26 days) diminishes the secondary paw swelling and inhibits heat-inactivated BCG induced-inflammtory polyarthritis[1].
Animal Model: | Rat carrageenan-induced edema model[1] | Dosage: | 5 mg/kg, 10 mg/kg, 20 mg/kg | Administration: | Gastrointestinal administration; 5-20 mg/kg; 1 hour before carrageenan injection | Result: | Inhibited the edema response with different doses. |
Animal Model: | Rat adjuvant-induced arthritis (AIA) model[1] | Dosage: | 5 mg/kg, 10 mg/kg, 20 mg/kg | Administration: | Gastrointestinal administration; 5-20 mg/kg; started on day 7; 26 days | Result: | Inhibited adjuvant-induced chronic inflammation at the doses of 10 and 20 mg/kg. |
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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(270.65 mM;Need ultrasonic) 配制储备液 1 mM | 2.7065 mL | 13.5325 mL | 27.0651 mL | 5 mM | 0.5413 mL | 2.7065 mL | 5.4130 mL | 10 mM | 0.2707 mL | 1.3533 mL | 2.7065 mL |
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此方案可获得 ≥ 2.08 mg/mL (5.63 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.63 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 20.8 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。
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