BAY 60-6583|cas:910487-58-0|西域试剂

BAY 60-6583,99.97%

产品编号：Bellancom-103171| CAS NO：910487-58-0| 分子式：C₁₉H₁₇N₅O₂S| 分子量：379.44

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货号	价格	库存与货期
Bellancom-103171	￥1100.00	杭州北京（现货）
Bellancom-103171	￥1400.00	杭州北京（现货）
Bellancom-103171	￥5500.00	杭州北京（现货）
Bellancom-103171	￥9900.00	杭州北京（现货）

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BAY 60-6583

产品介绍

BAY 60-6583 是腺苷 A2B受体 的高效选择性激动剂，对 A2B 受体 (EC₅₀= 3 nM) 的选择性高于 A1，A2A 和 A3 受体。BAY 60-6583 可以与小鼠，兔和狗 A2BAR 结合，K_i 值分别为 750 nM，340 nM 和 330 nM。BAY 60-6583 在心肌缺血模型中具有心脏保护作用。

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^[5].

体外研究

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^[4].
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^[4].

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

Cell Cycle Analysis^[4]

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^[4]

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^[5].

西域 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.

体内研究

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (263.55 mM; Need ultrasonic)

配制储备液

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

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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: ≥ 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 ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 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。