计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
Information
S-(+)-Rolipram inhibits human monocyte cyclic AMP-specificPDE4withIC50of 0.75 μM, has anti-inflammatory and anti-depressant activity in the central nervous system, less potent than its R enantiomer.
In vitro
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 [Cip1] and p27 [Kip1], 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
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.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥100%
规格
英文别名
(4S)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone
规格或纯度
10mM in DMSO
英文名称
S-(+)-Rolipram
生化机理
S-(+)-Rolipram 可抑制人单核细胞环 AMP 特异性 PDE4，其 IC50 值为 0.75 μM，在中枢神经系统中具有抗炎和抗抑郁活性，但药效低于其 R 对映体。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激活剂
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=C(C=C(C=C1)[C@@H]2CC(=O)NC2)OC3CCCC3
PubChem CID
分子量
275.34
Reaxy-Rn
6687797
技术文档
高级数据
关联靶点（人）
PDE4D
Tclin
cAMP特异性3'，5'-环磷酸二酯酶4D(cAMP-specific 3',5'-cyclic phosphodiesterase 4D)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 74 mg/mL (199.78 mM); Water: Insoluble; Ethanol: Insoluble;
比旋光度
32° (C=0.5,MeOH)
熔点
134 °C
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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