(S)-4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone
S- (+)-Rolipram
CAS: 85416-73-5
Molecular Formula: C16H21NO3
(S)-4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone - Names and Identifiers
(S)-4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone - Physico-chemical Properties
| Molecular Formula | C16H21NO3 |
| Molar Mass | 275.34 |
| Density | 1.155 |
| Melting Point | 133-136℃ |
| Appearance | White to off-white solid. |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| In vitro study | S-( )-Rolipram acts on human monocytes to inhibit LPS-induced TNFα expression by inhibiting PDE4 with an IC50 of 2 μm. 1 μm S-( )-Rolipram significantly resists ovalbumin (OA)-induced concentration-related contraction of tracheal cartilage rings, this tracheal cartilage ring was isolated from a guinea pig sensitive to OA. S-( )-Rolipram inhibited PDE4 activity in PDE-4a cell line stably expressing recombinant full-length human CHO-K1 with IC50 of 450 nM. Treatment of the human glioma cell line A- 172 with Rolipram (including the R-and S-enantiomers of Rolipram) increases the expression of the cell cycle inhibitors p21(Cip1) and p27(Kip1), and reducing cdk2 activity, which is an essential cyclin-dependent kinase in cell cycle progression. As A result, the proliferation of A- 172 cells was inhibited, and the cell cycle was stopped at G1 phase. Finally, A- 172 of the cells treated with roripram underwent differentiation followed by apoptosis. S-( )-Rolipram acts on human monocytes to inhibit LPS-induced TNFα expression by inhibiting PDE4 with an IC50 of 2 μm. 1 μm S-( )-Rolipram significantly resists ovalbumin (OA)-induced concentration-related contraction of tracheal cartilage rings, this tracheal cartilage ring was isolated from a guinea pig sensitive to OA. S-( )-Rolipram inhibited PDE4 activity in PDE-4a cell line stably expressing recombinant full-length human CHO-K1 with IC50 of 450 nM. Treatment of the human glioma cell line A- 172 with Rolipram (including the R-and S-enantiomers of Rolipram) increases the expression of the cell cycle inhibitors p21(Cip1) and p27(Kip1), and reducing cdk2 activity, which is an essential cyclin-dependent kinase in cell cycle progression. As A result, the proliferation of A- 172 cells was inhibited, and the cell cycle was stopped at G1 phase. Finally, A- 172 of the cells treated with roripram underwent differentiation followed by apoptosis. |
| In vivo study | S-( )-Rolipram reduces OA-induced bronchoconstriction in anesthetized guinea pigs sensitive to OA with an ID50 of 0.25 mg/kg,S-( )-Rolipram had no effect on bronchoconstriction induced by intravenous injection of histamine and leukotriene d4-since S-( )-Rolipram abolished the response to OA. Higher dose (3-10 mg/kg) treatment reduced histamine but not leukotriene d4-induced bronchoconstriction. Pretreatment of conscious OA-sensitive guinea pigs in the stomach with S-( )-Rolipram, reduced OA-induced specific conductance reduction by bronchoalveolar lavage and histological evaluation, the corresponding lung eosinophil influx was also reduced, and this effect was dose-dependent. S-( )-Rolipram reduces OA-induced bronchoconstriction in anesthetized guinea pigs sensitive to OA with an ID50 of 0.25 mg/kg,S-( )-Rolipram had no effect on bronchoconstriction induced by intravenous injection of histamine and leukotriene d4-since S-( )-Rolipram abolished the response to OA. Higher dose (3-10 mg/kg) treatment reduced histamine but not leukotriene d4-induced bronchoconstriction. Pretreatment of conscious OA-sensitive guinea pigs in the stomach with S-( )-Rolipram, reduced OA-induced specific conductance reduction by bronchoalveolar lavage and histological evaluation, the corresponding lung eosinophil influx was also reduced, and this effect was dose-dependent. |
(S)-4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 3.632 ml | 18.159 ml | 36.319 ml |
| 5 mM | 0.726 ml | 3.632 ml | 7.264 ml |
| 10 mM | 0.363 ml | 1.816 ml | 3.632 ml |
| 5 mM | 0.073 ml | 0.363 ml | 0.726 ml |
Last Update：2024-01-02 23:10:35
(S)-4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone - Reference Information
| biological activity | S- ( )-Rolipram inhibits human monocyte ring AMP-specific PDE4,IC50 is 0.75 μM, acts on the central nervous system, has anti-inflammatory and antidepressant activities, and is slightly weaker than its R-enantiomer effect. S-( )-Rolipram inhibits PDE4,IC50 of 0.75 μM, which is specific for cyclic AMP of human monocytes. It acts on the central nervous system and has anti-inflammatory and antidepressant activities, slightly weaker than its R-enantiomer effect. |
| in vitro study | S-( )-Rolipram acts on human monocytes, inhibiting LPS-induced TNFα expression by inhibiting PDE4, IC50 is 2 μM. 1 μM S-( )-Rolipram significantly resists ovalbumin (OA)-induced contraction of the tracheal cartilage ring, which was isolated from OA-sensitive guinea pigs. S-( )-Rolipram acts on CHO-K1 cell lines stably expressing recombinant full-length human PDE-4a, inhibiting PDE4 activity with IC50 of 450 nM. Treatment of human glioma cell line A- 172 with Rolipram (including Rolipram R-and S-enantiomers) increases the expression of cell cycle inhibitors p21(Cip1) and p27(Kip1) and reduces cdk2 activity, which is an essential cell cycle protein-dependent kinase in cell cycle progression. As a result, the proliferation of A- 172 cells was inhibited and the cell cycle stopped at G1 phase. Finally, Rolipram-treated A- 172 cells undergo differentiation and subsequent apoptosis. S-( )-Rolipram acts on human monocytes and inhibits LPS-induced TNFα expression by inhibiting PDE4 with IC50 of 2 μM. 1 μM S-( )-Rolipram significantly resists ovalbumin (OA)-induced contraction of the tracheal cartilage ring, which was isolated from OA-sensitive guinea pigs. S-( )-Rolipram acts on CHO-K1 cell lines stably expressing recombinant full-length human PDE-4a, inhibiting PDE4 activity with IC50 of 450 nM. Treatment of human glioma cell line A- 172 with Rolipram (including Rolipram R-and S-enantiomers) increases the expression of cell cycle inhibitors p21(Cip1) and p27(Kip1) and reduces cdk2 activity, which is an essential cell cycle protein-dependent kinase in cell cycle progression. As a result, the proliferation of A- 172 cells was inhibited and the cell cycle stopped at G1 phase. Finally, Rolipram-treated A- 172 cells undergo differentiation and subsequent apoptosis. |
| in vivo study | S-( )-Rolipram treated anesthetized guinea pigs sensitive to OA to reduce OA-induced bronchial shrinkage, ID50 is 0.25 mg/kg,S-( )-Rolipram has no effect on bronchial shrinkage induced by intravenous histamine and leukotriene D4, because S-( )-Rolipram abolishes the response to OA. Higher dose (3-10 mg/kg) treatment reduced histamine instead of leukotriene D4-induced bronchial shrinkage. Using S-( )-Rolipram to pretreat guinea pigs that are consciously sensitive to OA in the stomach, by bronchoalveolar lavage and histological evaluation, OA-induced specific conductance reduction and corresponding pulmonary eosinophil influx are reduced. This effect is dose-dependent. S-( )-Rolipram treatment of anesthetized OA-sensitive guinea pigs reduced OA-induced bronchial shrinkage with ID50 of 0.25 mg/kg. S-( )-Rolipram had no effect on bronchial shrinkage induced by intravenous histamine and leukotriene D4-, because S-( )-Rolipram abolished the response to OA. Higher dose (3-10 mg/kg) treatment reduced histamine instead of leukotriene D4-induced bronchial shrinkage. Using S-( )-Rolipram to pretreat guinea pigs that are consciously sensitive to OA in the stomach, by bronchoalveolar lavage and histological evaluation, OA-induced specific conductance reduction and corresponding pulmonary eosinophil influx are reduced. This effect is dose-dependent. |
| target | TargetValue PDE4 0.75 μM |
| Target | Value |
| PDE4 | 0.75 μM |
Last Update：2024-04-09 19:05:05
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Product Name: S- (+)-Rolipram Visit Supplier Webpage Request for quotation
CAS: 85416-73-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 85416-73-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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