ROLIPRAM
Background- Product Name
- ROLIPRAM
- CAS No.
- 61413-54-5
- Chemical Name
- ROLIPRAM
- Synonyms
- 4-(3-(CYCLOPENTYLOXY)-4-METHOXYPHENYL)PYRROLIDIN-2-ONE;SB 95952;ROLIPRAM;ZK-62711;Roliprame;(¨¤)-Rolipr;Rolipram >(±)-Rolipram;ROLIPRAM 98+%;(R,S)-Rolipram
- CBNumber
- CB2703866
- Molecular Formula
- C16H21NO3
- Formula Weight
- 275.34
- MOL File
- 61413-54-5.mol
ROLIPRAM Property
- 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
- pka
- 16.02±0.40(Predicted)
- color
- white to off-white
- biological source
- synthetic (organic)
- Water Solubility
- H2O: 0.2mg/mL
ethanol: 7mg/mL
DMSO: 7.3mg/mL - 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.
- InChI
- 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)
- InChIKey
- HJORMJIFDVBMOB-UHFFFAOYSA-N
- SMILES
- O(C1CCCC1)C1C=C(C2CC(NC2)=O)C=CC=1OC
Safety
- 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
- Storage Class
- 11 - Combustible Solids
- Toxicity
- LD50 oral in mouse: > 300mg/kg
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
P405Store locked up.
N-Bromosuccinimide Price
- Product number
- R6520
- Product name
- Rolipram
- Purity
- solid, ≥98% (HPLC)
- Packaging
- 10mg
- Price
- $194
- Updated
- 2026/03/19
- Product number
- 557330
- Product name
- Rolipram
- Packaging
- 5mg
- Price
- $253
- Updated
- 2026/03/19
- Product number
- R0110
- Product name
- Rolipram
- Purity
- >98.0%(HPLC)
- Packaging
- 50mg
- Price
- $178
- Updated
- 2026/03/19
- Product number
- R0110
- Product name
- Rolipram
- Purity
- >98.0%(HPLC)
- Packaging
- 250mg
- Price
- $617
- Updated
- 2026/03/19
- Product number
- 10011132
- Product name
- Rolipram
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $29
- Updated
- 2024/03/01
ROLIPRAM Chemical Properties,Usage,Production
Description
Rolipram (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 Properties
Yellowish solid
Uses
antipsychotic
Uses
A selective, cell permeable inhibitor of cAMP-specific phosphodiesterase (PDE4).
Uses
Pharmacological tool for characterization of phosphodiesterase isoenzymes.
Uses
(±)-Rolipram is a cAMP-specific phosphodiesterase 4 (PDE4) inhibitor.
Definition
ChEBI: 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 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.
Biological Activity
Selective 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 Actions
Cell permeable: yes
storage
Room temperature
Background
The small-molecule Rolipram is an inhibitor of phosphodiesterase 4, which catalyzes the hydrolysis of cyclic-AMP to regulate cellular responses to a number of extracellular signals. Rolipram inhibits multiple isozymes of PDE4, including PDE4A, PDE4B, and PDE4D. Treatment of myeloid cells with Rolipram resulted in phosphorylation of cAMP-response element-binding protein and implied the presence of both high and low affinity components. Rolipram and other phosphodiesterase inhibitors were seen as having potential therapeutic benefits in preclinical models of psychiatric and neurologic diseases. Unfortunately, severe dose-limiting side effects limited the clinical application of PDE inhibitors. Still, Rolipram treatment in a mouse model of intracerebral hemorrhage demonstrated some neuroprotective benefits through activation of the cAMP/AMPK/SIRT1 pathway. Rolipram treatment of fibroblasts from ligamentum flavum hypertrophy patients inhibited PDE4A and PDE4B activity, blocked TGF-β1 by restoring p-ERK1/2 expression, and inhibited expression of fibrosis-related proteins.
References
[1] M L REEVES P J E B K Leigh. 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 inhibitors.[J]. Biochemical Journal, 1987, 241 2: 535-541. DOI:10.1042/bj2410535
[2] AKINORI NISHI. Distinct roles of PDE4 and PDE10A in the regulation of cAMP/PKA signaling in the striatum.[J]. Journal of Neuroscience, 2008, 28 42: 10460-10471. DOI:10.1523/jneurosci.2518-08.2008
[3] S.H. CHRISTIANSEN . Combined anti-inflammatory effects of β2-adrenergic agonists and PDE4 inhibitors on astrocytes by upregulation of intracellular cAMP[J]. Neurochemistry international, 2011, 59 6: Pages 837-846. DOI:10.1016/j.neuint.2011.08.012
ROLIPRAM Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from ROLIPRAM manufacturers
- Product
- rolipram 61413-54-5
- Price
- US $15.00-10.00/KG
- Min. Order
- 1KG
- Purity
- 99%+ HPLC
- Supply Ability
- Monthly supply of 1 ton
- Release date
- 2021-06-26
- Product
- ROLIPRAM 61413-54-5
- Price
- US $1.00/KG
- Min. Order
- 1KG
- Purity
- 99%
- Supply Ability
- 200kgs
- Release date
- 2020-02-14