SB 239063 是一种有效、选择性、可口服的p38 MAPK抑制剂，对重组纯化的人 p38α 的IC50值为 44 nM，对 p38α 和 p38β 的活性等效，但对 p38γ 或 p38δ 无所用。具有抗哮喘作用，还被用于增强因衰老或疾病受损的记忆，如阿尔茨海默病。
| 生物活性 | SB 239063 is a potent, selective and orally activep38 MAPKinhibitor, exhibits anIC50of 44 nM for recombinant purified humanp38α, with equipotent inhibitory activity againstp38αandp38β. SB 239063 has no effect onp38γorp38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD[1][2]. |
| IC50& Target | IC50: 44 nM (Human p38α)[1] |
体外研究
(In Vitro) | SB 239063 (0.1–10 μM ; 29 hours, 47 hours) increases apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards[1].
SB 239063 potently inhibits IL-1 and TNF- a production in LPS-stimulated human peripheral blood monocytes with IC50values of 120 nM and 350 nM, respectively[1].
Apoptosis Analysis[1] | Cell Line: | Eosinophils (guinea pig BALs) | | Concentration: | 0.1μM, 1μM, 10μM | | Incubation Time: | 29 hours, 47 hours | | Result: | Increased apoptosis of eosinophils in a dose-related in the presence of 10 pM IL-5 at every time point from 21 hours onwards. |
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体内研究
(In Vivo) | SB 239063 (12 mg/kg; p.o.; 1 hour before and 4 hours after OA challenge; b.i.d. for 3 days) significantly inhibits the resultant antigen-induced airway eosinophilia[1].
SB 239063 (12 mg/kg; p.o.) almost abolishes ovalbumin (OA)-induced airway eosinophilia (~ 93% inhibition) by inhalation[1].
SB 239063 is a potent inhibitor of LPS-induced TNF-alpha production in the mouse peritoneal cavity with an EC50of 5.8 mg/kg (2.8–10.3; 95% CL)[1].
| Animal Model: | Male BALB/c mice (18–20 g)[1] | | Dosage: | 12 mg/kg | | Administration: | Oral administration; 1 h before and 4 h after OA challenge; bis in die for 3 days | | Result: | Significantly inhibited the resultant antigen-induced airway eosinophilia. |
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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(90.47 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7144 mL | 13.5722 mL | 27.1444 mL | | 5 mM | 0.5429 mL | 2.7144 mL | 5.4289 mL | | 10 mM | 0.2714 mL | 1.3572 mL | 2.7144 mL |
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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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.79 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.79 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 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: ≥ 2.5 mg/mL (6.79 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.79 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。
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