CGH 2466 dihydrochloride
目录号 : GC14674
adenosine receptor antagonist
Cas No.:1177618-54-0
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
CGH 2466 dihydrochloride is a combined adenosine receptor antagonist. It is an inhibitor of phosphodiesterase type 4 and p38 mitogen-activated protein kinase. It inhibited the phosphodiesterase 4D (PDE4D) isoenzyme with an IC50 value of 22±5 nM. It inhibited the p38 mitogen-activated protein (MAP) kinases α and β with IC50 values of 187±18, 400±38 nM, respectively [1].
There are four adenosine receptor subtypes of the G protein-coupled receptor family, designated as A1, A2A, A2B and A3 [2]. Adenosine plays a role in the control of inflammation [3]. Phosphodiesterases can inactivate cAMP. In inflammatory cells, phosphodiesterase-4 (PDE4) is the predominant isoenzyme [4]. In mammalian cells, the p38 MAPK was thought to be important for regulating cellular responses during infection via its effects on the expression of proinflammatory molecules [5].
CGS15943 is a broad spectrum adenosine antagonist, SB203580 is a prototypical inhibitor of the p38 MAP kinase, and cilomilast is a standard inhibitor of PDE4. Data showed that CGH2466 was similar to SB203580 in potency as a p38 MAP kinase inhibitor, and was similar to cilomilast in activity to inhibit PDE4D. Compared to CGS15943, CGH 2466 showed similar potency to inhibit A1, A2B and A3 adenosine receptors. In contrast to CGS15943, CGH2466 was not active at the A2A receptor. Compared with other above compounds, CGH2466 was an inhibitor of the highest potency to inhibit selected enzymes or receptors in leucocyte-based assays [1].
48 h after the allergen challenge, bronchoalveolar lavage recovered eosinophil numbers. In sensitized mice, aerosol challenge of ovalbumin was able to increase these eosinophil numbers. In this animal model of asthmatic inflammation, 15 min before and 24 h after the challenge, the intranasal administration of CGH2466, dose-dependently inhibited the airway eosinophilia induced by ovalbumin, reaching significant levels at doses of 3 and 10 mg.kg-1 [1].
References:
[1]. Trifilieff A, Keller TH, Press NJ, et al. CGH2466, a combined adenosine receptor antagonist, p38 mitogen‐activated protein kinase and phosphodiesterase type 4 inhibitor with potent in vitro and in vivo anti‐inflammatory activities. British journal of pharmacology, 2005, 144(7): 1002-1010.
[2]. Klotz KN, Hessling J, Hegler J, et al. Comparative pharmacology of human adenosine receptor subtypes-characterization of stably transfected receptors in CHO cells. Naunyn-Schmiedeberg's archives of pharmacology, 1997, 357(1): 1-9.
[3]. Yang D, Zhang Y, Nguyen HG, et al. The A2B adenosine receptor protects against inflammation and excessive vascular adhesion. The Journal of clinical investigation, 2006, 116(7): 1913-1923.
[4]. Gamble E, Grootendorst DC, Brightling CE, et al. Antiinflammatory effects of the phosphodiesterase-4 inhibitor cilomilast (Ariflo) in chronic obstructive pulmonary disease. American journal of respiratory and critical care medicine, 2003, 168(8): 976-982.
[5]. Han J, Jiang Y, Li Z, et al. Activation of the transcription factor MEF2C by the MAP kinase p38 in inflammation. 1997, 386(6622):296-299.
| Cas No. | 1177618-54-0 | SDF | |
| 化学名 | 4-(3,4-dichlorophenyl)-5-(pyridin-4-yl)thiazol-2(3H)-imine dihydrochloride | ||
| Canonical SMILES | ClC1=C(Cl)C=C(C(NC2=N)=C(S2)C3=CC=NC=C3)C=C1 | ||
| 分子式 | C14H9N3SCl2.2HCl | 分子量 | 395.13 |
| 溶解度 | <3.95mg/ml in DMSO; <1.98mg/ml in ethanol | 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 | 2.5308 mL | 12.6541 mL | 25.3081 mL |
| 5 mM | 0.5062 mL | 2.5308 mL | 5.0616 mL |
| 10 mM | 0.2531 mL | 1.2654 mL | 2.5308 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。