YM 90709|163769-88-8|-陌孚医药/Medlife

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YM 90709

目录号: PC15187 纯度: ≥98%

CAS No. :163769-88-8

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中文名称

YM 90709

中文别名

5,6-二氢-2,3-二甲氧基-6,6-二甲基苯并[7,8]吲哚嗪并[2,3-B]喹喔啉;5,6-二氢-2,3-二甲氧基-6,6-二甲基苯并[7,8]吲哚烷并[2,3-b]喹噁啉

英文名称

2,3-Dimethoxy-6,6-dimethyl-5,6-dihydrobenzo(7,8)indolizino (2,3-b)quinoxaline

英文别名

2,3-Dimethoxy-6,6-dimethyl-5,6-dihydrobenzo[7,8]indolizino[2,3-b]quinoxaline;Benz[7,8]indolizino[2,3-b]quinoxaline,5,6-dihydro-2,3-dimethoxy-6,6-dimethyl-;YM 90709;YM-90709;Bio-0867;Tocris-1675;5,6-DIHYDRO-2,3-DIMETHOXY-6,6-DIMETHYLBENZ[7,8]INDOLIZINO[2,3-B]QUINOXALINE;YM90709;BAS 00454872;Oprea1_619477;Oprea1_183698;GTPL5090;HMS3676B08;HMS3412B08;HMS3268M17;BCP17183;2,3-dimethoxy-6,6-dimethyl-5,6-dihydrobenzo(7,8)indolizino (2,3-b)qu;2,3-Dimethoxy-6,6-dimethyl-5,6-dihydrobenzo(7,8)indolizino (2,3-b)quinoxaline

Cas No.

163769-88-8

分子式

C₂₂H₂₁N₃O₂

分子量

359.42

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

YM-90709 is a novel IL-5 inhibitor which selectively blocks the binding of IL-5 to the IL-5 receptor (IL-5R).YM-90709 potently inhibits the binding of [I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells with IC₅₀ values of 1.0 and 0.57 μM.

性状

Solid

IC50 & Target[1][2]

IL-5

体外研究(In Vitro)

YM-90709 (0-100 μM;1 hour) inhibits the binding of [I]-IL-5 to IL-5R on human peripheral eosinophils and eosinophilic HL-60 clone 15 cells.
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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	Purified eosinophils were suspended at 5×10 cells/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

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.

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Inbred female Brown-Norway (BN) rats and used at 4-6 weeks of age.
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Morokata T, et al. Characterization of YM-90709 as a novel antagonist which inhibits the binding of interleukin-5 to interleukin-5 receptor. Int Immunopharmacol. 2002 Nov;2(12):1693-702. [Information]

[2]. Morokata T, et al. Effect of a novel interleukin-5 receptor antagonist, YM-90709, on antigen-induced eosinophil infiltration into the airway of BDF1 mice. Immunol Lett. 2005 Apr 15;98(1):161-5. [Information]

溶解度数据

体外研究:

DMSO : 62.5 mg/mL (173.89 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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