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61413-54-5

中文名称 诺普利兰
英文名称 ROLIPRAM
CAS 61413-54-5
分子式 C16H21NO3
分子量 275.34
MOL 文件 61413-54-5.mol
更新日期 2024/03/22 13:03:25
61413-54-5 结构式 61413-54-5 结构式

基本信息

中文别名
咯利普兰
诺普利兰
英文别名
SB 95952
ZK-62711
ROLIPRAM
Roliprame
ROLIPRAM 98+%
(R,S)-Rolipram
Rolipram, >=97%
ZK-62711, SB95952, ME-3167
4-(3-(cyclopentyloxy)-4-methoxyphenyl)-2-pyrrolidinon
4-(3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL)PYRROLIDIN-2-ONE
所属类别
生物化工:PDE 抑制剂

物理化学性质

熔点127-133 °C
熔点127-133 °C
沸点418.29°C (rough estimate)
密度1.0677 (rough estimate)
折射率1.5500 (estimate)
储存条件0-6°C
储存条件Sealed in dry,Store in freezer, under -20°C
溶解度H2O: 0.2 mg/mL
溶解度在水中的溶解度0.2 mg/mL
酸度系数(pKa)16.02±0.40(Predicted)
形态solid
颜色white to off-white
Merck14,8251
稳定性可在-20°C下的DMSO或乙醇溶液保存长达3个月。

安全数据

危险性符号(GHS)
GHS07
警示词警告
危险性描述H315-H319-H335
危险品标志Xi
危险类别码36/37/38-11
危险类别码36/37/38-11
安全说明26-36
安全说明26-36
危险品运输编号3249
WGK Germany3
WGK Germany3
RTECS号UY5749237
危险等级6.1(b)
包装类别III
海关编码29337900
毒性LD50 oral in mouse: > 300mg/kg

常见问题列表

生物活性
PDE4的选择性抑制剂,Rolipram (ZK-62711, SB 95952),抑制免疫纯化的PDE4B和PDE4D活性,IC50分别为130 nM和240 nM。具有抗炎活性。
靶点
TargetValue
PDE4B
(Cell-free assay)
130 nM
PDE4D
(Cell-free assay)
240 nM
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.

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