BAY 60-6583|910487-58-0|-陌孚医药/Medlife

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BAY 60-6583

目录号: PC10995 纯度: ≥98%

CAS No. :910487-58-0

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中文名称

BAY 60-6583

英文名称

BAY 60-6583

英文别名

BAY 60-6583;2-[6-amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]pyridin-2-yl]sulfanylacetamide;2-[[6-Amino-3,5-dicyano-4-[4-(cyclopropylmethoxy)phenyl]-2-pyridinyl]thio]-acetamide;BAY 60–6,583;BAY 606583;BAY606583;BR 4887;BR4887

Cas No.

910487-58-0

分子式

C₁₉N₅O₂SH₁₇

分子量

379.44

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

BAY 60-6583 is a potent and high-affinity agonist of adenosine A_2B receptor (EC₅₀ = 3 nM) over A1, A2A, and A3 receptors. BAY 60-6583 binds to mouse, rabbit, and dog A2BAR with K_i values of 750 nM, 340 nM and 330 nM, respectively. BAY 60-6583 has a cardioprotective effect in a myocardial ischemia model.

性状

Solid

体外研究(In Vitro)

BAY 60-6583 exhibits EC₅₀ values for receptor activation >10,000 nM for both A1 and A2A AR and 3 nM for A2B AR subtype in CHO cells expressing recombinant human A1, A2A or A2B ARs.
BAY 60-6583(0-10 μM) exhibits the maximum agonist effect of BAY in the absence of siRNA is 68 %, which is significantly different from that in the presence of 5, 50 and 500 nM siRNA (54%, 48% and 36%, respectively). It exhibits EC₅₀ values of BAY in the absence and presence siRNA with 98±22, 102±17, 127±31 and 93±19 nM, respectively, in T24 cells.
BAY 60-6583 (5 μM; 24 hours) increases the accumulation of cells at the G1 phase with a decrease in G2/M phase in RAW264.7 preosteoclasts.
BAY 60-6583 (5 μM; 24 hours) specifically inhibits the activation of Akt by M-CSF, whereas M-CSF-induced ERK1/2 activation is not affected by BAY 60-6583 treatment in RAW264.7 preosteoclasts.

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

Cell Cycle Analysis

Cell Line:	RAW264.7 preosteoclasts
Concentration:	5 μM
Incubation Time:	48 hours
Result:	Caused an arrest of cells at the G1 phase.

Western Blot Analysis

Cell Line:	RAW264.7 preosteoclasts
Concentration:	5 μM
Incubation Time:	48 hours
Result:	Exhibited an inhibition of M-CSF-mediated Akt activation and resulted in the decrease of osteoclast proliferation.

体内研究(In Vivo)

BAY 60-6583 (intravenous injection; 100 mcg/kg) reduces the infarction area just prior to reperfusion in ischaemic rabbit hearts.
BAY 60-6583 (intraperitoneal injection; 2 mg/kg) attenuates LPS-induced lung injury, pre-treatment with this compound can significantly decrease LPS-increased IL-6 levels in WT-mice, In contrast, BAY 60-6583 treatment is ineffective in abrogating these inflammatory parameters in A2BAR mice.
BAY 60-6583 (intratumoral administration) causes a significant increase in tumor-infiltrating MDSCs, it does not affect neither their ability to suppress T-cell proliferation nor their degree of maturation, it also stimulates the production of IL-10 and CCL2 in the tumor tissue.

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

Animal Model:	A2BAR mice on a C57BL/6J mice
Dosage:	2 mg/kg
Administration:	Intraperitoneal injection; 2 mg/kg
Result:	Demonstrated attenuation of lung inflammation and pulmonary edema in wild-type but not in gene-targeted mice for the A2BAR.

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]. Aherne CM, et al. Epithelial-specific A2B adenosine receptor signaling protects the colonic epithelial barrier during acute colitis.Mucosal Immunol. 2015 Nov;8(6):1324-38. [Information]

[2]. Schingnitz U, et al. Signaling through the A2B adenosine receptor dampens endotoxin-induced acute lung injury.J Immunol. 2010 May 1;184(9):5271-9. [Information]

[3]. Gao ZG, et al. Probing biased/partial agonism at the G protein-coupled A(2B) adenosine receptor.Biochem Pharmacol. 2014 Aug 1;90(3):297-306. [Information]

[4]. Yoon Taek Oh, et al. A2B Adenosine Receptor Stimulation Down-regulates M-CSF-mediated Osteoclast Proliferation. Biomed Sci Letters 2017;23:194-200

[5]. John A. Auchampach, et al. Characterization of the A2B Adenosine Receptor from Mouse, Rabbit, and Dog. J Pharmacol Exp Ther. 2009 Apr;329(1):2-13. [Information]

[6]. Morello S1, et al. Targeting the adenosine A2b receptor in the tumor microenvironment overcomes local immunosuppression by myeloid-derived suppressor cells.Oncoimmunology. 2014 Feb 14;3:e27989. eCollection 2014. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (263.55 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	2.6355 mL	13.1773 mL	26.3546 mL
5 mM	0.5271 mL	2.6355 mL	5.2709 mL
10 mM	0.2635 mL	1.3177 mL	2.6355 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: ≥ 4.17 mg/mL (10.99 mM); Clear solution

此方案可获得 ≥ 4.17 mg/mL (10.99 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 41.7 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% corn oil
Solubility: ≥ 4.17 mg/mL (10.99 mM); Clear solution

此方案可获得 ≥ 4.17 mg/mL (10.99 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 41.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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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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