中文名 | 咯利普兰 |
英文名 | Rolipram |
别名 | 诺普利兰 咯利普兰 咯利普兰(消旋) ROLIPRAM 咯利普兰 诺普利兰, 一种PDE4抑制剂 4-[3-(环戊氧基)-4-甲氧基苯基]吡咯-2-酮 |
英文别名 | ZK 62711 SB 95952 Rolipram Roliprame Rolipramum BRN 1588548 (R,S)-Rolipram UNII-K676NL63N7 Rolipramum [Latin] 4-(3-Cyclopentyloxy-4-methoxyphenyl)-2-pyrrolidone 4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one 4-[3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL]-2-PYRROLIDINONE 4-(3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL)PYRROLIDIN-2-ONE 4-(3-(Cyclopentyloxy)-4-methoxyphenyl)-2-pyrrolidinone 2-Pyrrolidinone, 4-(3-(cyclopentyloxy)-4-methoxyphenyl)- 2-Pyrrolidinone, 4-[3-(cyclopentyloxy)-4-methoxyphenyl]- (4S)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one (4R)-4-[3-(cyclopentyloxy)-4-methoxyphenyl]pyrrolidin-2-one 4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone, ZK62711 |
CAS | 61413-54-5 |
EINECS | 262-771-1 |
化学式 | C16H21NO3 |
分子量 | 275.34 |
InChI | InChI=1/C16H21NO3/c1-19-14-7-6-11(12-9-16(18)17-10-12)8-15(14)20-13-4-2-3-5-13/h6-8,12-13H,2-5,9-10H2,1H3,(H,17,18)/t12-/m0/s1 |
密度 | 1.0677 (rough estimate) |
熔点 | 127-133 °C |
沸点 | 418.29°C (rough estimate) |
闪点 | 239.7°C |
蒸汽压 | 4.17E-09mmHg at 25°C |
溶解度 | H2O: 0.2mg/ml |
折射率 | 1.5500 (estimate) |
酸度系数 | 16.02±0.40(Predicted) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
稳定性 | 从提供的购买之日起稳定2年。DMSO或乙醇中的溶液可以在-20 °C下储存长达3个月。 |
敏感性 | Sensitive to heat |
外观 | 固体 |
颜色 | white to off-white |
Merck | 14,8251 |
MDL号 | MFCD00270906 |
体外研究 | 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. |
体内研究 | 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. |
危险品标志 | Xi - 刺激性物品 |
风险术语 | R36/37/38 - 刺激眼睛、呼吸系统和皮肤。 R11 - 高度易燃。 |
安全术语 | S26 - 不慎与眼睛接触后,请立即用大量清水冲洗并征求医生意见。 S36 - 穿戴适当的防护服。 |
危险品运输编号 | 3249 |
WGK Germany | 3 |
RTECS | UY5749237 |
海关编号 | 29337900 |
Hazard Class | 6.1(b) |
Packing Group | III |
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