GS-6201
(Synonyms: 3-乙基-1-丙基-8-(1-(3-(三氟甲基)苄基)-1H-吡唑-4-基)-1H-嘌呤-2,6(3H,8H)-二酮,CVT-6883) 目录号 : GC38789
An adenosine A2B receptor antagonist
Cas No.:752222-83-6
Sample solution is provided at 25 µL, 10mM.
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CVT-6883 is an adenosine A2B receptor antagonist (Ki = 22 nM).1 It is selective for adenosine A2B over adenosine A1, A2A, and A3 receptors (Kis = 1,940, 3,280, and 1,070 nM, respectively), as well as a panel of 84 receptors, ion channels, transporters, and enzymes at 10 ?M. CVT-6883 (6 mg/kg) decreases allergen challenge-induced bronchoalveolar lavage fluid (BALF) eosinophil and lymphocyte infiltration and airway reactivity in a mouse model of allergic asthma.2 It also decreases fibrosis in the non-infarct zone, improves ejection fractions, and reduces ventricular tachycardia in a rat model of myocardial infarction.3
1.Elzein, E., Kalla, R.V., Li, X., et al.Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseasesJ. Med. Chem.51(7)2267-2278(2008) 2.Mustafa, S.J., Nadeem, A., Fan, M., et al.Effect of a specific and selective A2B adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthmaJ. Pharmacol. Exp. Ther.320(3)1246-1251(2007) 3.Zhang, H., Zhong, H., Everett, T.H., 4th, et al.Blockade of A2B adenosine receptor reduces left ventricular dysfunction and ventricular arrhythmias 1 week after myocardial infarction in the rat modelHeart Rhythm11(1)101-109(2014)
| Cas No. | 752222-83-6 | SDF | |
| 别名 | 3-乙基-1-丙基-8-(1-(3-(三氟甲基)苄基)-1H-吡唑-4-基)-1H-嘌呤-2,6(3H,8H)-二酮,CVT-6883 | ||
| Canonical SMILES | O=C(N(CCC)C1=O)N(CC)C(C1=N2)=NC2C3=CN(N=C3)CC4=CC=CC(C(F)(F)F)=C4 | ||
| 分子式 | C21H21F3N6O2 | 分子量 | 446.43 |
| 溶解度 | DMSO : 100 mg/mL (224.00 mM; ultrasonic and warming and heat to 60°C) | 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 | 2.24 mL | 11.2 mL | 22.3999 mL |
| 5 mM | 0.448 mL | 2.24 mL | 4.48 mL |
| 10 mM | 0.224 mL | 1.12 mL | 2.24 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
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet