557330
Rolipram
≥98% (HPLC), cAMP-specific phosphodiesterase inhibitor, solid
别名:
Rolipram, 4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone
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关于此项目
经验公式（希尔记法）:
C16H21NO3
化学文摘社编号:
分子量:
275.34
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
产品名称
Rolipram, A cell-permeable, selective inhibitor of cAMP-specific phosphodiesterase (PDE IV; IC₅₀ = 800 nM).
SMILES string
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 key
HJORMJIFDVBMOB-UHFFFAOYSA-N
description
Merck USA index - 14, 8251
assay
≥98% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
color
white
solubility
DMSO: soluble
shipped in
ambient
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
PDE IV
PDE IV
Product does not compete with ATP.
Reversible: no
Target IC50: 800 nM against cAMP-specific phosphodiesterase (PDE IV)
Disclaimer
Toxicity: Irritant (B)
General description
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.
Other Notes
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.
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.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). DMSO stock solutions are stable for up to 6 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
Sriram Hemachandran et al.
Frontiers in cellular neuroscience, 18, 1363219-1363219 (2024-05-02)
Cochlear afferent synapses connecting inner hair cells to spiral ganglion neurons are susceptible to excitotoxic trauma on exposure to loud sound, resulting in a noise-induced cochlear synaptopathy (NICS). Here we assessed the ability of cyclic AMP-dependent protein kinase (PKA) signaling
H Ji
Methods in molecular medicine, 51, 363-377 (2001-01-01)
Angiotensin type-1 receptors (AT(1) receptors) mediate various physiological actions of angiotensin (Ang II) via multiple-signal transduction pathways (1). In addition to the phospholipase C pathway and dihydropyridine-sensitive voltage-dependent calcium channels, AT(1) receptors can couple to inhibition of adenylate cyclase via
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