MRS1523
目录号 : GC14078An adenosine A3 receptor antagonist
Cas No.:212329-37-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ki = 18.9 nM for human adenosine A3 receptor
Ki = 113 nM for rat adenosine A3 receptor
MRS1523 is a selective adenosine A3 receptor (A3R) antagonist. A3R is strongly overexpressed in cancer cell lines and cancer tissues. The activation of the A3R is related to several second messenger systems which are for signaling pathways including asthmatic, inflammatory, and ischemic responses.
In vitro: MRS1523 reversed the increase in mRNA expression in B16-F10 Melanoma Cells. Also, MRS1523 antagonized the modulation in the expression level of the proteins, which indicated that adenosine A3R mediated the responses [1].
In vivo: C57BL/6J, male mice, inoculated B16-F10 melanoma cells, were administered MRS1523 at a dose of 100 μg/kg orally twice daily for 15 days. MRS1523 counteracted the activity of IB-MECA which is an adenosine A3R agonist. In addition, it was demonstrated that the response was adenosine A3R mediated. The modulation of up-regulation of GSK-3β expression level was neutralized by MRS1523, further suggesting the specificity of the response [1].
Reference:
[1]. Madi, L., Rosenberg-Haggen, B., Nyska, A., & Korenstein, R. Enhancing pigmentation via activation of A3 adenosine receptors in B16 melanoma cells and in human skin explants. Experimental Dermatology. 2012; 22(1): 74-77.
| Cas No. | 212329-37-8 | SDF | |
| 化学名 | 6-ethyl-5-[(ethylthio)carbonyl]-2-phenyl-4-propyl-3-pyridinecarboxylic acid propyl ester | ||
| Canonical SMILES | CCCOC(C1=C(CCC)C(C(SCC)=O)=C(CC)N=C1C2=CC=CC=C2)=O | ||
| 分子式 | C23H29NO3S | 分子量 | 399.5 |
| 溶解度 | ≤50mg/ml in DMSO;50mg/ml in dimethyl formamide | 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 | 2.5031 mL | 12.5156 mL | 25.0313 mL |
| 5 mM | 0.5006 mL | 2.5031 mL | 5.0063 mL |
| 10 mM | 0.2503 mL | 1.2516 mL | 2.5031 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。