(R,S)-Rolipram, Inhibitor of PDE IV

SKU
R-1012
  • CAS:61413-54-5
  • Formula:C16H21NO3
  • MW:275.4 Da
  • Appearance:White solid
  • Purity:≥98%

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Product Name Qty
(R,S)-Rolipram, Inhibitor of PDE IV
5 mg
$41.66
(R,S)-Rolipram, Inhibitor of PDE IV
50 mg
$196.33

Rolipram is a selective phosphodiesterase-4 inhibitor discovered and developed by Schering AG as a potential antidepressant drug in the early 1990s. It was previously used as an antideppresant but was discontinued because of its serious side effects. Rolipram has shown to boost the levels of NMNAT2 (Nicotinamide mononeucleotide adenylyl transferase 2), an enzyme that blocks the processes associated with dementia - a form of Alzheimers. In other studies it has shown to breakdown misfolded tau proteins.

More Information
Alternate Name/Synonyms
ZK-62711
SKU
R-1012
CAS #
61413-54-5
Chemical Name
4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidin-2-one
Chemical Formula
C16H21NO3
Molecular Weight
275.4 Da
Appearance
White solid
Purity
≥98%
Solubility
Soluble in Water
Melting Point
132°C
Preparation
N/A
Storage Temp
4°C, desiccated
THERAPEUTIC AREA
Neurodegenrative Diseases
USE
Rolipram is a selective, cell-permeable inhibitor of cAMP-specific PDE (phosphodiesterase) (PDE4, IC50=1 μM). This compound has been shown to inhibit PDE4 activity in human cavernosal tissue, which interrupts the signal transduction pathway of erectile response. Rolipram promotes apoptosis in HL60 cells through a cAMP-independent mechanism and has been shown to enhance neuronal survival. Rolipram is an inhibitor of PDE4A1 and PDE4B.
Merck Index
13.8332.2001
MDL NUMBER
MFCD00270906
CHEMACX
X1038250-2
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)
SMILES
COc1ccc(cc1OC2CCCC2)C3CC(=O)NC3
RTECS
UY5749237
Handling
Further processing of solid materials may result in the formation of combustible dusts. The potential for combustible dust formation should be taken into consideration before additional processing occurs. Provide appropriate exhaust ventilation at places where dust is formed.
Citations
BEHAVIORAL/SYSTEMS/COGNITIVE: Phosphodiesterase-4D Knock-Out and RNA Interference-Mediated Knock-Down Enhance Memory and Increase Hippocampal Neurogenesis via Increased cAMP Signaling Yun-Feng Li, Yu-Fang Cheng, Ying Huang, Marco Conti, Steven P. Wilson, James M. O'Donnell, and Han-Ting Zhang J. Neurosci., Jan 2011; 31: 172 - 183.
Citations_Hyperlink
http://www.jneurosci.org/cgi/reprint/31/1/172
msds 1
/media/upload/pdf/R-1012, Rolipram, SDS, diamond format.pdf
Certificate of Analysis 1
/media/upload/pdf/R-1012, F1254E.pdf
Certificate of Analysis 2
/media/upload/pdf/R-1012, F1254D.pdf
Certificate of Analysis 3
/media/upload/pdf/R-1012, F1254C.pdf
Handling Further processing of solid materials may result in the formation of combustible dusts. The potential for combustible dust formation should be taken into consideration before additional processing occurs. Provide appropriate exhaust ventilation at places where dust is formed.
Citations Treating rheumatoid arthritis to target: 2014 update of the recommendations of an international task force
A long lasting β1 adrenergic receptor stimulation of cAMP/protein kinase A (PKA) signal in cardiac myocytes
Peripheral phosphodiesterase 4 inhibition produced by 4-[2-(3,4-Bis-difluoromethoxyphenyl)-2-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-phenyl]-ethyl]-3-methylpyridine-1-oxide (L-826,141) prevents experimental autoimmune encephalomyelitis
Phosphodiesterase 4B is an effective therapeutic target in colorectal cancer
Assays for Cyclic Nucleotide‐Specific Phosphodiesterases (Families 1 to 5)
Assays for Cyclic Nucleotide-Specific Phosphodiesterases (Families 1 to 5)
Inhibition of phosphodiesterase 4D decreases the malignant properties of DLD‑1 colorectal cancer cells by repressing the AKT/mTOR/Myc signaling pathway
Recovery from paralysis in adult rats using embryonic stem cells
Phosphodiesterase 4 inhibition but not beta-adrenergic stimulation suppresses tumor necrosis factor-alpha release in peripheral blood mononuclear cells in septic shock
Tissue plasminogen activator expression and barrier properties of human brain microvascular endothelial cells
cAMP promotes neurite outgrowth and extension through protein kinase A but independently of Erk activation in cultured rat motoneurons
Neuroanatomical and pharmacological assessment of Fos expression induced in the rat brain by the phosphodiesterase-4 inhibitor 6-(4-pyridylmethyl)-8-(3-nitrophenyl) quinoline
The phosphodiesterase-4 inhibitor rolipram attenuates heroin-seeking behavior induced by cues or heroin priming in rats
Molecular therapeutic targets in rheumatoid arthritis
Cloning and characterization of novel PDE4D isoforms PDE4D6 and PDE4D7
Long-term viral brain-derived neurotrophic factor delivery promotes spasticity in rats with a cervical spinal cord hemisection
Inhibition of phosphodiesterase-4 decreases ethanol intake in mice
Derivation of high purity neuronal progenitors from human embryonic stem cells
Protection against doxorubicin cardiomyopathy in rats: role of phosphodiesterase inhibitors type 4
Phosphodiesterase inhibitor modulation of brain microvascular endothelial cell barrier properties
Effect of xiaoyaosan decoction on learning and memory deficit in rats induced by chronic immobilization stress
A novel diet-induced murine model of steatohepatitis with fibrosis for screening and evaluation of drug candidates for nonalcoholic steatohepatitis
Vasopressin regulation of inner medullary collecting ducts and compensatory changes in mice lacking adenosine A1 receptors
The peripheral nervous system: injury and disease
Effect of Delayed Rolipram on Thermal Hyperalgesia Following Spinal Cord Injury
The phosphodiesterase-4 (PDE4) inhibitor rolipram decreases ethanol seeking and consumption in alcohol-preferring Fawn-Hooded rats
Synthesis and Biological Activity of Chalcone Derivatives as Anti - Asthmatics Agents
The phosphodiesterase-4 inhibitor roflumilast decreases ethanol consumption in C57BL/6J mice
A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening
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