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(S)-(+)-咯利普兰 /(S)-(+)-Rolipram {[allProObj[0].p_purity_real_show]}

货号:A107169 同义名: S-(+)-Rolipram;(+)-Rolipram

(S)-(+)-Rolipram is a PDE4-inhibitor and an anti-inflammatory agent, less potent than its R-enantiomer.

(S)-(+)-Rolipram 化学结构 CAS号:85416-73-5
(S)-(+)-Rolipram 化学结构
CAS号:85416-73-5
(S)-(+)-Rolipram 3D分子结构
CAS号:85416-73-5
(S)-(+)-Rolipram 化学结构 CAS号:85416-73-5
(S)-(+)-Rolipram 3D分子结构 CAS号:85416-73-5
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(S)-(+)-Rolipram 纯度/质量文件 产品仅供科研

货号:A107169 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PDE PDE1 PDE10A PDE2 PDE3 PDE4 PDE5 PDE6 其他靶点 纯度
Doxofylline 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

99+%
7-(2,3-Dihydroxypropyl)theophylline 98%
Aminophylline +

PDE, IC50: 0.12 mM

98+%
Anagrelide HCl 99%+
Irsogladine AChR,mAChR 98%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

99%+
Dipyridamole 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

97%
Luteolin +

PDE1, Ki: 15.0 μM

++

PDE2, Ki: 6.4 μM

+

PDE3, Ki: 13.9 μM

+

PDE4, Ki: 11.1 μM

+

PDE5, Ki: 9.5 μM

98%
Milrinone ++

PDE2, IC50: 5.2 μM

++

PDE3, IC50: 2.1 μM

ATPase 98%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

98%
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

98%
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A4, IC50: 4.3 nM

PDE4A1, IC50: 0.7 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

98+%
Avanafil ++++

PDE5, IC50: 1 nM

98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

98%
Icariin ++

PDE5, IC50: 0.432 μM

98%
Sildenafil +++

PDE6, IC50: 33 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

(S)-(+)-Rolipram 生物活性

靶点
  • PDE4

    PDE4, IC50:0.75 μM

描述 (S)-(+)-Rolipram, known as (+)-Rolipram, is a selective inhibitor of cyclic AMP (cAMP)-specific phosphodiesterase 4 (PDE4) with an IC50 of 1100 nM. It is effective in suppressing tumor necrosis factor-alpha (TNFα) production in human mononuclear cells[1].[2].[3].
体内研究

Moreover, (+)-Rolipram (0.025-6.25 mg/kg; a single i.p. injection) reduces locomotor activity and induces head twitches in rats in a dose-dependent manner[2].

In further studies, (+)-Rolipram (0.06-25 mg/kg; a single i.p. injection) leads to a dose-related decrease in the rectal temperature of rats[2].

体外研究

In laboratory settings, (+)-Rolipram (0.015-1000 μM; 20 h) has shown a dose-dependent ability to inhibit LPS-induced TNF production in human mononuclear cells, with an IC50 value of 550 nM[1].

(S)-(+)-Rolipram 参考文献

[1]Semmler J, et, al. The specific type IV phosphodiesterase inhibitor rolipram suppresses tumor necrosis factor-alpha production by human mononuclear cells. Int J Immunopharmacol. 1993 Apr;15(3):409-13.

[2]Wachtel H. Neurotropic effects of the optical isomers of the selective adenosine cyclic 3',5'-monophosphate phosphodiesterase inhibitor rolipram in rats in-vivo. J Pharm Pharmacol. 1983 Jul;35(7):440-4.

[3]Ortmann R, et, al. Rolipram forms a potent discriminative stimulus in drug discrimination experiments in rats. Psychopharmacology (Berl). 1986;89(3):273-7.

(S)-(+)-Rolipram 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.63mL

0.73mL

0.36mL

18.16mL

3.63mL

1.82mL

36.32mL

7.26mL

3.63mL

(S)-(+)-Rolipram 技术信息

CAS号85416-73-5
分子式C16H21NO3
分子量 275.343
别名 S-(+)-Rolipram;(+)-Rolipram;(S)-Rolipram
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(381.34 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 7 mg/mL clear

PO 0.5% CMC-Na 47 mg/mL suspension

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