ROLIPRAM

ROLIPRAM Basic information
Product Name:ROLIPRAM
Synonyms:ROLIPRAM 98+%;Roliprame;2-Pyrrolidinone, 4-[3-(cyclopentyloxy)-4-methoxyphenyl]-;SB 95952;4-[3-(Cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone, ZK62711;4-[3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL]-2-PYRROLIDINONE;(R,S)-Rolipram;ZK-62711, SB95952, ME-3167
CAS:61413-54-5
MF:C16H21NO3
MW:275.34
EINECS:262-771-1
Product Categories:Inhibitor;DIPIPERON;Inhibitors;Antineoplastic;Cyclic Nucleotide related;Signalling
Mol File:61413-54-5.mol
ROLIPRAM Structure
ROLIPRAM Chemical Properties
Melting point 127-133 °C
Boiling point 418.29°C (rough estimate)
density 1.0677 (rough estimate)
refractive index 1.5500 (estimate)
storage temp. Sealed in dry,Store in freezer, under -20°C
solubility H2O: 0.2 mg/mL
form solid
pka16.02±0.40(Predicted)
color white to off-white
Merck 14,8251
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.
Safety Information
Hazard Codes Xi
Risk Statements 36/37/38-11
Safety Statements 26-36
RIDADR 3249
WGK Germany 3
RTECS UY5749237
HazardClass 6.1(b)
PackingGroup III
HS Code 29337900
ToxicityLD50 oral in mouse: > 300mg/kg
MSDS Information
ProviderLanguage
ACROSEnglish
SigmaAldrichEnglish
ROLIPRAM Usage And Synthesis
DescriptionRolipram (61413-54-5) is a selective inhibitor of cAMP-specific phosphodiesterase (PDE4), IC50 = 1 μM. Displays beneficial effects in neurodegenerative diseases. Rolipram also displays anti-inflammatory activity and synergizes with forskolin (cat.# 10-2073). Cell permeable.
Chemical PropertiesYellowish solid
Uses(±)-Rolipram is a cAMP-specific phosphodiesterase 4 (PDE4) inhibitor.
UsesPharmacological tool for characterization of phosphodiesterase isoenzymes.
UsesA selective, cell permeable inhibitor of cAMP-specific phosphodiesterase (PDE4).
Usesantipsychotic
DefinitionChEBI: Rolipram is a member of the lclass of pyrrolidin-2-ones that is pyrrolidin-2-one bearing a 3-(cyclopentyloxy)-4-methoxyphenyl substituent at the 4-position. It is a type IV-specific phosphodiesterase (PDE4) inhibitor. It has a role as an antidepressant and an EC 3.1.4.* (phosphoric diester hydrolase) inhibitor.
General DescriptionA 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.
Biological ActivitySelective inhibitor of cAMP phosphodiesterase (PDE4) (IC 50 = 2.0 μ M). Discriminates between two conformational states of PDE4 isoenzymes. See separate isomers ((R)-(-)-Rolipram and (S)-(+)-Rolipram).
Biochem/physiol ActionsCell permeable: yes
References1) Reeves et al. (1987), The identification of a new cyclic nucleotide phosphodiesterase activity in human and guinea-pig cardiac ventricle. Implications for the mechanism of action of selective phosphodiesterase; Biochem. J., 241 535 2) Nishi et al. (2008), Distinct Roles of PDE4 and PDE10A in the Regulation of cAMP/PKA Signaling in the Striatum; J. Neurosci., 28 10460 3) Christiansen et al. (2011), Combined anti-inflammatory effects of β2-adrenergic agonists and PDE4 inhibitors on astrocytes by upregulation of intracellular cAMP; Neurochem. Int., 59 837
ROLIPRAM Preparation Products And Raw materials

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