Powder: -20°C for 3 years | In solvent: -80°C for 1 year
(S)-(+)-Rolipram ((+)-Rolipram) 是一种 cAMP 依赖性磷酸二酯酶 4 (PDE4) 抑制剂,IC50=1100 nM。它能够抑制人单核细胞产生的肿瘤坏死因子 α (TNFα)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 198 | 现货 | ||
5 mg | ¥ 469 | 现货 | ||
10 mg | ¥ 813 | 现货 | ||
25 mg | ¥ 1,360 | 现货 | ||
50 mg | ¥ 1,980 | 现货 | ||
100 mg | ¥ 2,960 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 459 | 现货 |
产品描述 | (S)-(+)-Rolipram ((+)-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. |
靶点活性 | PDE4:0.75 μM |
体外活性 | S-(+)-Rolipram suppresses LPS-induced TNFα expression from human monocyte through inhibiting PDE4 with IC50 about 2 μM. [1] 1 μM S-(+)-Rolipram significantly antagonizes ovalbumin (OA) induced concentration-related contractions of tracheal rings which are isolated from OA-sensitized guinea pigs. [2] 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. [3] 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. [4] |
体内活性 | 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. [2] |
别名 | (S)-Rolipram, (+)-Rolipram, 盐酸环胞苷, S- (+)-Rolipram |
分子量 | 275.34 |
分子式 | C16H21NO3 |
CAS No. | 85416-73-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 27.5 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.6319 mL | 18.1594 mL | 36.3187 mL | 90.7968 mL |
5 mM | 0.7264 mL | 3.6319 mL | 7.2637 mL | 18.1594 mL | |
10 mM | 0.3632 mL | 1.8159 mL | 3.6319 mL | 9.0797 mL | |
20 mM | 0.1816 mL | 0.908 mL | 1.8159 mL | 4.5398 mL | |
50 mM | 0.0726 mL | 0.3632 mL | 0.7264 mL | 1.8159 mL | |
100 mM | 0.0363 mL | 0.1816 mL | 0.3632 mL | 0.908 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
(S)-(+)-Rolipram 85416-73-5 Apoptosis Metabolism PDE TNFα (S)-Rolipram Rolipram tumor inhibit (S)(+)Rolipram (+)-Rolipram mononuclear phosphodiesterase 盐酸环胞苷 (S) (+) Rolipram Phosphodiesterase (PDE) cAMP S- Rolipram Inhibitor S- (+)-Rolipram factor necrosis inhibitor