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| 品牌 | absin | CAS | 85416-73-5 |
|---|---|---|---|
| 分子式 | C16H21NO3 | 纯度 | 98% |
| 分子量 | 275.34 | 货号 | abs47028335 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | monocyte cyclic AMP-specific PDE4 with I | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
S- (+)-Rolipram 85416-73-5
| 产品描述 | |
| 描述 | S-(+)-Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | (S)-(+)-咯利普兰；(+)-Rolipram；(S)-Rolipram |
| 外观 | 类白色粉末 |
| 可溶性/溶解性 | DMSO : 27.5 mg/mL (100 mM) |
| 生物活性 | |
| 靶点 | PDE4 |
| In vitro(体外研究) | S-(+)-Rolipram suppresses LPS-induced TNFα expression from human monocyte through inhibiting PDE4 with IC50 about 2 μM. 1 μM S-(+)-Rolipram significantly antagonizes ovalbumin (OA) induced concentration-related contractions of tracheal rings which are isolated from OA-sensitized guinea pigs. S-(+)-Rolipram inhibits PDE4 activity in a CHO-K1 cell line which stably expresses a recombinant full length human PDE-4a with IC50 at 450 nM. Treatment of the human glioma cell line A-172 with Rolipram (including both R- and S-enantiomers of Rolipram) results in increased expression of the cell cycle inhibitors p21 and p27 , and decreased activity of cdk2, a cyclindependent kinase essential for cell cycle progression. As a result, the proliferation of A-172 cells is inhibited, with induction of a G1 block. Eventually, Rolipram-treated A-172 cells undergo differentiation, which is followed by apoptotic cell death. |
| In vivo(体内研究) | In anesthetized, ventilated OA-sensitive guinea pigs, S-(+)-Rolipram reduces OA-induced bronchoconstriction with ID50 values of approximately 0.25 mg/kg i.v. Histamine- and leukotriene D4-induced bronchoconstriction are not affected by doses of S-(+)-Rolipram which abolishes the response to OA. Higher doses (3-10 mg/kg) reduce histamine-, but not the leukotriene D4-induced bronchoconstriction. In conscious OA-sensitive guinea pigs, intragastric pretreatment with S-(+)-Rolipram dose-dependently reduces both the OA-induced decreases in specific conductance as well as the corresponding pulmonary eosinophil influx as assessed by both bronchoalveolar lavage and histological evaluation. |
| 参考文献 | |
| 参考文献 |
| 研究领域 | |
| 研究领域 | Signal TransductionSecond MessengerNucleotide MessengercAMP Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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