YM-90709 是一种常规的IL-5阻断剂，选择性的抑制 IL-5 与 IL-5 受体结合。YM-90709 能有效抑制 [125I]-IL-5 与 IL-5R 在人外周嗜酸性粒细胞和嗜酸性 HL-60 克隆 15 细胞上的结合，IC50值分别为 1.0 和 0.57 μM。
| 生物活性 | YM-90709 is a novelIL-5inhibitor which selectively blocks the binding ofIL-5to theIL-5 receptor(IL-5R).YM-90709 potently inhibits the binding of [125I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells withIC50values of 1.0 and 0.57 μM[1]. |
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体外研究
(In Vitro) | YM-90709 (0-100 μM;1 hour) inhibits the binding of [125I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells[1].
YM-90709 (0-100 μM; 96 hour; Eosinophilic HL-60 clone 15 cells) affects IL-5 and GM-CSF and prolonged the survival time of eosinophils[1].
YM-90709 (0-100 μM; 5 min; Eosinophilic HL-60 clone 15 cells) inhibits IL-5-induced, but not GM-CSF-induced, eosinophil survival as well as the tyrosine phosphorylation of Janus kinase 2[2].
Cell Viability Assay[1] | Cell Line: | Purified eosinophils were suspended at 5×105cells/ml in RPMI-1640 medium. | | Concentration: | 0.01, 0.1, 1, 10 and 100 μM | | Incubation Time: | 96 hours | | Result: | The survival time of eosinophils was prolonged. |
Western Blot Analysis[1] | Cell Line: | Eosinophilic HL-60 clone 15 cells in RPMI-1640 medium containing 10% FBS, antibiotics, 50 mM 2-ME and 25 mM HEPPES. | | Concentration: | | | Incubation Time: | 5 min | | Result: | Reduced the IL-5-induced phosphorylation of JAK2 to near basal levels. |
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体内研究
(In Vivo) | YM-90709 (0.01-10 mg/kg; intravenous injection, 72 hours, Inbred female Brown-Norway (BN) rats) results in the inhibition of antigen-induced infiltration of eosinophils and lymphocytes, but not neutrophils or monocytes, into the bronchoalveolar lavage fluid (BALF) of Brown-Norway (BN) rats[2].
| Animal Model: | Inbred female Brown-Norway (BN) rats and used at 4-6 weeks of age[2]. | | Dosage: | 0.01, 0.1, 1, 10 mg/kg | | Administration: | Intravenous injection; 72 hours | | Result: | Inhibited WBC and eosinophil infiltration in a dose-dependent manner. |
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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 : 62.5 mg/mL(173.89 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7823 mL | 13.9113 mL | 27.8226 mL | | 5 mM | 0.5565 mL | 2.7823 mL | 5.5645 mL | | 10 mM | 0.2782 mL | 1.3911 mL | 2.7823 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 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.79 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.79 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% (20%SBE-β-CDin saline) Solubility: 2.08 mg/mL (5.79 mM); Suspended solution; Need ultrasonic
此方案可获得 2.08 mg/mL (5.79 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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