S- (+)-Rolipram

S- (+)-Rolipram ((+)-Rolipram) 是一种环状 AMP(cAMP) 特异性磷酸二酯酶 4 (PDE4) 抑制剂，IC50 为 1100 nM。

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5mg

￥412.00

330.00

- +
10mg

￥775.00

620.00

- +
25mg

￥1650.00

1320.00

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50mg

￥2825.00

2260.00

- +

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货号: ajci4396
CAS: 85416-73-5
别名: (+)-Rolipram; (S)-Rolipram
分子式: C16H21NO3
分子量: 275.34
纯度: >98%
溶解度: ≥ 13.9 mg/mL in DMSO, ≥ 20.76 mg/mL in EtOH with ultrasonic and warming
储存: Store at -20°C
库存: 现货

Background

(S)-(+)-Rolipram is a PDE4-inhibitor and an anti-inflammatory agent, less potent than its R enantiomer.Target: PDE4B; PDE4DRolipram, a selective inhibitor of the cyclic AMP-specific phosphodiesterase (PDE IV). Rolipram did not inhibit 5-lipoxygenase activity but did inhibit human monocyte production of leukotriene B4 (LTB4, IC50 3.5 microM). Rolipram inhibited arachidonic acid-induced inflammation in the mouse, while the low Km-cyclic-GMP PDE inhibitor. Rolipram had a modest effect on LTB4 production in the mouse, but markedly reduced LTB4-induced PMN infiltration [1]. In humans and animals rolipram produces thereby a variety of biological effects. These effects include attenuation of endogenous depression and inflammation in the central nervous system (CNS), both effects are of potential clinical relevance [2].

参考文献:
[1]. Griswold, D.E., et al., Effect of selective phosphodiesterase type IV inhibitor, rolipram, on fluid and cellular phases of inflammatory response. Inflammation, 1993. 17(3): p. 333-44.
[2]. Zhu, J., E. Mix, and B. Winblad, The antidepressant and antiinflammatory effects of rolipram in the central nervous system. CNS Drug Rev, 2001. 7(4): p. 387-98.
[3]. MacKenzie SJ, et al. Action of rolipram on specific PDE4 cAMP phosphodiesterase isoforms and on the phosphorylation of cAMP-response-element-binding protein (CREB) and p38 mitogen-activated protein (MAP) kinase in U937 monocyticcells. Biochem J. 2000 Apr 15;347(Pt 2):571-8.
[4]. Korhonen R, et al. Attenuation of TNF production and experimentally induced inflammation by PDE4 inhibitor rolipram is mediated by MAPK phosphatase-1. Br J Pharmacol. 2013 Aug;169(7):1525-36.