CDP 840 hydrochloride
(Synonyms: GR259653X) 目录号 : GC16632
CDP 840 hydrochloride (GR259653X) 是一种有效的、选择性的和口服活性的磷酸二酯酶 IV (PDE IV) 抑制剂。
Cas No.:162542-90-7
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
CDP 840 is a selective phosphodiesterase type IV (PDE4) inhibitor [1] [2] [3] with an IC50 value of 0.007 µM [4].
PDE4 is most abundantly distributed in inflammatory cells such as monocytes and macrophages [3]. PDE4 is a high-affinity cAMP-selective isozyme. It was found that PDE4 was in almost all cell types in asthma pathogenesis [2].
CD P840 showed a potent inhibition against PDE4 with IC50 values ranging from 2-30 nM to different isoenzymes of PDE4. There are four expressed PDE4 isoenzymes in baculovirus cells, i.e. PDE4A, PDE4B, PDE4C and PDE4D. Except for PDE4C2, CDP 840 did not exhibit isoform selectivity of PDE4. CD P840 exhibited a hill number of about 1.0 against all four PDE4 isoenzymes. For all four PDE4 isoenzymes, CDP 840 acted as a simple competitive inhibitor [5].
In vivo, CDP 840 (30 mg/kg) increased cAMP by 145% in the hippocampus and by 112% in the prefrontal cortex of male Sprague-Dawley rats. CDP 840 at doses of 10 and 30 mg/kg increased the phosphorylation of cAMP response element binding protein (pCREB) in the hippocampus (by 36 and 55%, respectively) and in the prefrontal cortex (by 32 and 60%, respectively). But these doses did not affect the expression of the cAMP response element binding protein (CREB). Repeated treatment with CDP 840 at a dose of 30 mg/kg increased the cell proliferation in rat hippocampus, but these cells were not survival [6].
References:
[1]. T.R. Jones, M. McAuliffe, C.S. McFarlane, et al. Effects of a selective phosphodiesterase IV inhibitor (CDP-840) in a leukotriene-dependent non-human primate model of allergic asthma. Can. J. Physiol. Pharmacol., 1998, 76: 210-217.
[2]. Chun Li, Nathalie Chauret, Laird A. Trimble, et al. Investigation of the in vitro metabolism profile of a phosphodiesterase-IV inhibitor, CDP-840: leading to structural optimization. Drug Metabolism and Disposition, 2001, 29:232–241.
[3]. John E. Souness and Sudha Rao. Proposal for Pharmacologically Distinct Conformers of PDE4 Cyclic AMP Phosphodiesterases. Cell. Signal., 1997, 9(3/4):227-236.
[4]. Christopher Hulme, Gregory B. Poli, Fu-Chih Huang, et al. Quaternary substituted PDE4 inhibitors I: the synthesis and in vitro evaluation of a novel series of oxindoles. Bioorganic & Medicinal Chemistry Letters, 1998, 8:175-178.
[5]. M.J. Perry, J. O'Connell, C. Walker, et al. CDP840: a novel inhibitor of PDE-4. Cell Biochem. Biophys., 1998, 29(1-2):113-32.
[6]. Lan Xiao, James P. O’Callaghan and James M. O’Donnell. Effects of Repeated Treatment with Phosphodiesterase-4 Inhibitors on cAMP Signaling, Hippocampal Cell Proliferation, and Behavior in the Forced-Swim Test. J. Pharmacol. Exp. Ther., 2011, 338(2):641-7.
| Cas No. | 162542-90-7 | SDF | |
| 别名 | GR259653X | ||
| 化学名 | (R)-4-(2-(3-(cyclopentyloxy)-4-methoxyphenyl)-2-phenylethyl)pyridine hydrochloride | ||
| Canonical SMILES | COC1=C(OC2CCCC2)C=C([C@](C3=CC=CC=C3)([H])CC4=CC=NC=C4)C=C1.Cl | ||
| 分子式 | C25H27NO2.HCl | 分子量 | 409.95 |
| 溶解度 | <40.99mg/ml in DMSO | 储存条件 | Desiccate at RT |
| 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 | 2.4393 mL | 12.1966 mL | 24.3932 mL |
| 5 mM | 0.4879 mL | 2.4393 mL | 4.8786 mL |
| 10 mM | 0.2439 mL | 1.2197 mL | 2.4393 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。