4-(3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL)PYRROLIDIN-2-ONE
Rolipram
CAS: 61413-54-5
Molecular Formula: C16H21NO3
4-(3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL)PYRROLIDIN-2-ONE - Names and Identifiers
4-(3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL)PYRROLIDIN-2-ONE - Physico-chemical Properties
| Molecular Formula | C16H21NO3 |
| Molar Mass | 275.34 |
| Density | 1.0677 (rough estimate) |
| Melting Point | 127-133 °C |
| Boling Point | 418.29°C (rough estimate) |
| Flash Point | 239.7°C |
| Solubility | Soluble in water (0.2 mg/mL ), DMSO (7.3 mg/ml ), ethanol (7 mg/ml warm), DMF (~10 m |
| Vapor Presure | 4.17E-09mmHg at 25°C |
| Appearance | solid |
| Color | white to off-white |
| Merck | 14,8251 |
| pKa | 16.02±0.40(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| Sensitive | Sensitive to heat |
| Refractive Index | 1.5500 (estimate) |
| MDL | MFCD00270906 |
| Use | A selective, cell permeable inhibitor of cAMP-specific phosphodiesterase (PDE4). |
| In vitro study | The PDE4 selective inhibitor, Rolipram, inhibits immunopurified PDE4B and PDE4D activities similarly, with IC 50 s of approx. 130 nM and 240 nM respectively. In contrast, Rolipram inhibits immunopurified PDE4A activity with a dramatically lower IC 50 of around 3 nM. Rolipram increases phosphorylation of cAMP-response-element-binding protein (CREB) in U937 cells in a dose-dependent fashion, which implies the presence of both high affinity (IC 50 approx. 1 nM) and low affinity (IC 50 approx. 120 nM) components. Rolipram dose-dependently inhibits the IFN-gamma-stimulated phosphorylation of p38 MAPK in a simple monotonic fashion with an IC 50 of approx. 290 nM. Rolipram is a selective PDE4 inhibitor that inhibits all PDE4 isoforms A, B, C and D. Rolipram inhibits LPS-induced TNF production in a dose-dependent manner (IC 50 25.9 nM), and maximal/submaximal inhibition is observed with 2 μM drug concentration in J774 cells. |
| In vivo study | TNF mRNA and protein expression is induced by LPS in peritoneal macrophages (PM) from WT mice, and that is clearly (by 74 and 63% for TNF mRNA and TNF protein, respectively) inhibited by Rolipram. LPS-induced TNF production is enhanced in PM from MKP-1(-/-) mice as compared to that in PM from WT mice, which is in line with the published results. Interestingly, the inhibition of TNF mRNA and protein expression by Rolipram is markedly attenuated in PM from MKP-1(-/-) mice and does not reach statistical significance. Repeated administration of Rolipram (1.25 mg/kg, i.p.) reduces the number of escape failures in learned helplessness rats. |
4-(3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL)PYRROLIDIN-2-ONE - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | R36/37/38 - Irritating to eyes, respiratory system and skin. R11 - Highly Flammable |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
| UN IDs | 3249 |
| WGK Germany | 3 |
| RTECS | UY5749237 |
| HS Code | 29337900 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
| Toxicity | LD50 oral in mouse: > 300mg/kg |
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CAS: 61413-54-5
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CAS: 61413-54-5
Tel: 0531-6780 8539
Email: raven@sdfousi.ltd
Spot supply
Product Name: Rolipram Visit Supplier Webpage Request for quotationCAS: 61413-54-5
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Product Name: Rolipram Request for quotation
CAS: 61413-54-5
Tel: 0531-6780 8539
Email: raven@sdfousi.ltd
CAS: 61413-54-5
Tel: 0531-6780 8539
Email: raven@sdfousi.ltd
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