MRS 1754
目录号 : GC13807
MRS 1754是一种选择性A2B腺苷受体拮抗剂。
Cas No.:264622-58-4
Sample solution is provided at 25 µL, 10mM.
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MRS 1754 is a selective A2B adenosine receptor antagonist [1]. MRS 1754 blocks adenosine binding to the A2B receptor, thereby inhibiting downstream signaling pathways mediated by the receptor (e.g., cAMP production and inflammatory cytokine release) [2]. MRS 1754 is commonly used in asthma and chronic obstructive pulmonary disease research [3-4].
In rat aortic vascular smooth muscle cells, MRS 1754 (0.1μM; 4d) significantly attenuated the decrease in [3H]thymidine incorporation induced by 2′,3′-cAMP [5]. In preglomerular vascular smooth muscle cells, MRS-1754 (100nM; 4d) inhibited the antiproliferative effect of adenosine [6].
In cecal ligation and puncture-induced sepsis mice model, MRS 1754 (0.5-10mg/kg; sc; 3d) treatment significantly improved the survival rate of mice [7]. In gut ischemia and reperfusion mice model, MRS 1754 (9.52μM/kg; iv; single injection) blocks A2B-type adenosine receptors, counteracting the protective effects of NECA on leukocyte-endothelial interactions and capillary perfusion [8].
References:
[1]. Ji X, Kim Y C, Ahern D G, et al. [3H] MRS 1754, a selective antagonist radioligand for A2B adenosine receptors[J]. Biochemical pharmacology, 2001, 61(6): 657-663.
[2]. Fogli E. Adenosine receptors modulation of inflammatory cells: the foam cells history[J]. 2010.
[3]. Haskó G, Linden J, Cronstein B, et al. Adenosine receptors: therapeutic aspects for inflammatory and immune diseases[J]. Nature reviews Drug discovery, 2008, 7(9): 759-770.
[4]. Fozard J R, Tigani B, Wolber C, et al. Modeling the response of the asthmatic airways to adenosine: Mechanisms and receptors[J]. Drug development research, 2003, 59(1): 23-29.
[5]. Jackson E K, Ren J, Gillespie D G. 2′, 3′-cAMP, 3′-AMP, and 2′-AMP inhibit human aortic and coronary vascular smooth muscle cell proliferation via A2B receptors[J]. American Journal of Physiology-Heart and Circulatory Physiology, 2011, 301(2): H391-H401.
[6]. Jackson E K, Gillespie D G, Dubey R K. 2′-AMP and 3′-AMP inhibit proliferation of preglomerular vascular smooth muscle cells and glomerular mesangial cells via A2B receptors[J]. The Journal of pharmacology and experimental therapeutics, 2011, 337(2): 444-450.
[7]. Belikoff B G, Hatfield S, Georgiev P, et al. A2B adenosine receptor blockade enhances macrophage-mediated bacterial phagocytosis and improves polymicrobial sepsis survival in mice[J]. The Journal of Immunology, 2011, 186(4): 2444-2453.
[8]. Zhou J, Zimmermann K, Krieg T, et al. Adenosine receptor activation improves microcirculation in experimental intestinal ischemia/reperfusion[J]. Clinical Hemorheology and Microcirculation, 2015, 59(3): 257-265.
MRS 1754是一种选择性A2B腺苷受体拮抗剂 [1]。MRS 1754阻断腺苷与A2B受体结合，从而抑制该受体介导的下游信号通路（例如cAMP生成和炎症细胞因子释放） [2]。MRS 1754常用于哮喘和慢性阻塞性肺病的研究 [3-4]。
在大鼠主动脉血管平滑肌细胞中，MRS 1754（0.1μM；4d）显著减弱了2′,3′-cAMP诱导的[3H]胸苷掺入的减少 [5]。在肾小球前血管平滑肌细胞中，MRS-1754（100nM；4d）抑制了腺苷的抗增殖作用 [6]。
在盲肠结扎穿刺诱发的脓毒症小鼠模型中，MRS 1754（0.5-10mg/kg；sc；3d）治疗显著提高了小鼠的存活率 [7]。在肠缺血再灌注小鼠模型中，MRS 1754（9.52μM/kg；iv；单次注射）阻断了A2B型腺苷受体，从而抵消了NECA对白细胞-内皮细胞相互作用和毛细血管灌注的保护作用 [8]。
| Cell experiment [1]: | |
Cell lines | Rat aortic vascular smooth muscle cells (AVSMCs) |
Preparation Method | For cell number experiments, cells were allowed to attach overnight, were growth-arrested for 48h, and were treated with 2′,3′-cAMP, AMPs, or adenosine, with or without MRS 1754, in DMEM containing 2.5% FCS. Treatments were repeated every 24h for 4 days. On day 5, cells were dislodged and counted with a Coulter counter. |
Reaction Conditions | 0.1μM; 4d |
Applications | MRS 1754 significantly attenuated the decrease in [3H]thymidine incorporation induced by 2′,3′-cAMP. |
| Animal experiment [2]: | |
Animal models | Cecal ligation and puncture (CLP)-induced sepsis mice model |
Preparation Method | Mice were subjected to CLP to induce multibacterial sepsis. Mice were treated with an A2BR antagonist (MRS 1754) injected subcutaneously once daily for 3 days, while control mice were given vehicle only (Lactated Ringer's with 5% glucose + imipenem). |
Dosage form | 0.5-10mg/kg; sc; 3d |
Applications | MRS 1754 treatment significantly improved the survival rate of mice. |
References: | |
| Cas No. | 264622-58-4 | SDF | |
| 化学名 | N-(4-cyanophenyl)-2-(4-(2,6-dioxo-1,3-dipropyl-2,3,6,7-tetrahydro-1H-purin-8-yl)phenoxy)acetamide | ||
| Canonical SMILES | O=C(N(C1=O)CCC)N(CCC)C2=C1NC(C(C=C3)=CC=C3OCC(NC4=CC=C(C#N)C=C4)=O)=N2 | ||
| 分子式 | C26H26N6O4 | 分子量 | 486.52 |
| 溶解度 | 15 mg/mL in DMSO，insoluble 0.1 mg/mL in Water | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0554 mL | 10.2771 mL | 20.5541 mL |
| 5 mM | 0.4111 mL | 2.0554 mL | 4.1108 mL |
| 10 mM | 0.2055 mL | 1.0277 mL | 2.0554 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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