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Merck
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主要文件

557330

Sigma-Aldrich

Rolipram

A cell-permeable, selective inhibitor of cAMP-specific phosphodiesterase (PDE IV; IC₅₀ = 800 nM).

别名:

Rolipram, 4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone

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About This Item

经验公式（希尔记法）:
C16H21NO3
CAS号:
61413-54-5
分子量:
275.34
MDL號碼:
MFCD00270906
分類程式碼代碼:
12352200
NACRES:
NA.77

品質等級

100

描述

Merck USA index - 14, 8251

化驗

≥98% (HPLC)

形狀

solid

製造商／商標名

Calbiochem®

儲存條件

OK to freeze

顏色

white

溶解度

DMSO: soluble

運輸包裝

ambient

儲存溫度

2-8°C

SMILES 字串

N1CC(CC1=O)c2cc(c(cc2)OC)OC3CCCC3

InChI

1S/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)

InChI 密鑰

HJORMJIFDVBMOB-UHFFFAOYSA-N

一般說明

A cell-permeable, selective inhibitor of cAMP-specific phosphodiesterase (PDE IV; IC50 = 800 nM). A rolipram-insensitive PDE IV subtype is also known to exist. Also inhibits NF-κB and NFAT activation in Jurkat and primary T cells.
Cell permeable, selective competitive inhibitor of cAMP-specific phosphodiesterase IV (IC50 = 800 nM). Rolipram does not inhibit PDE I or PDE II, even at concentrations as high as 100 µM. It is only a weak inhibitor of PDE III (IC50 = 100 µM). A rolipram-insensitive phosphodiesterase IV subtype is also known to exist.

生化／生理作用

Cell permeable: yes
Primary Target
PDE IV
Product does not compete with ATP.
Reversible: no
Target IC50: 800 nM against cAMP-specific phosphodiesterase (PDE IV)

警告

Toxicity: Irritant (B)

重構

Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 6 months at -20°C.

其他說明

Navarro, J., et al. 1998. J. Virol. 72, 4712.
Truong, V.H. and Muller, T. 1994. FEBS Lett.353, 113.
Underwood, D.C., et al. 1994. J. Pharmacol. Exp. Ther. 270, 250.
Moore, J.B., Jr., et al. 1991. Biochem. Pharmacol.42, 679.
Reeves, M.L., et al. 1987. Biochem. J. 241, 535.
Schneider, H.H., et al. 1986. Eur. J. Pharmacol.127, 105.

法律資訊

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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Line M Grønning et al.
FEBS letters, 580(17), 4126-4130 (2006-07-11)
Overexpression of forkhead transcription factor FOXC2 in white adipose tissue (WAT) leads to a lean phenotype resistant to diet-induced obesity. This is due, in part, to enhanced catecholamine-induced cAMP-PKA signaling in FOXC2 transgenic mice. Here we show that rolipram treatment

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