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Stock availabilitIn Stock
In Stock
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CAS number
61413-54-5
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Description
Autophagy inhibitor
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Molecular weight
275,35 g/mol
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Primary research fields
Cancer, Autophagy
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Other name
4-(3-(Cyclopentyloxy)-4-methoxyphenyl)pyrrolidin-2-one
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Product category
Small Molecules
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Product type
Inhibitor
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Chemical formula
C16H21NO3
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Origin
Synthetic
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Purity pourcentage
>98% (TLC); NMR (Conforms)
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Soluble in
Soluble to 75 mM in DMSO and to 75 mM in ethanol.
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Physical appearance
White to off-white solid.
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Storage recommendations
-20ºC
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Shipping recommendations
Shipped Ambient
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Safety information
Classification: D2B- Toxic Material Causing Other Toxic Effects, Moderate skin irritant, Moderate respiratory irritant, Moderate eye irritant Safety Phrases: S22 - Do not breathe dust. S24/25 - Avoid contact with skin and eyes. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. Hazard statements: H315- Causes skin irritation. H319- Causes serious eye irritation. H335- May cause respiratory irritation. Precautionary statements: P261- Avoid breathing dust/ fume/ gas/ mist/ vapours/ spray. P264- Wash skin thoroughly after handling. P271- Use only outdoors or in a well-ventilated area. P280- Wear protective gloves/ eye protection/ face protection. P302 + P352- IF ON SKIN: Wash with plenty of soap and water. P304 + P340- IF INHALED: Remove victim to fresh air and keep at rest in a position comfortable for breathing. P305 + P351 + P338- IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. P312- Call a POISON CENTER or doctor/ physician if you feel unwell. P321- Specific treatment (see supplemental first aid instructions on this label). P332 + P313- If skin irritation occurs: Get medical advice/ attention. P337 + P313- If eye irritation persists: Get medical advice/ attention. P362- Take off contaminated clothing and wash before reuse. P403 + P233- Store in a well-ventilated place. Keep container tightly closed. P405- Store locked up. P501- Dispose of contents/ container to an approved waste disposal plant.
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PubChem number
5092
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Scientific context
Rolipram has been observed to selectively inhibit cAMP-phosphodiesterase (PDE4) by recruiting PDE4 into cytosolic aggregates that are not membrane-encapsulated. A down-stream effect of this observation is the inhibition of autophagy. Under normal conditions, autophagosomes are coated with the autophagic marker light chain 3 (LC3). LC3 binds directly to p62 protein, which shuttles protein to aggresomes, eventually leading to an autophagic event. In the absence of LC3, protein aggregates will not undergo autophagy, and will remain as cytosolic aggregates, as seen with the inhibition of PDE4 by Rolipram.
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Bibliography
1. Kato H., et al. (1995) Eur J Pharmacol. 272(1): 107-10. 2. Christian F., et al. (2010) Cell Signal. 22(10): 1576-96. 3. Houslay M.D., & Christian F. (2010) Autophagy. 6(8): 1198-200.
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Release date
31-Mar-2014
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PubMed number
Refer to PubMed
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Tested applications
To be tested
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Tested reactivity
To be tested
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Representative figure legend
Chemical structure of Rolipram (SIH-401), a Autophagy inhibitor. CAS #: 61413-54-5 . Molecular Formula: C16H21NO3. Molecular Weight: 275.35 g/mol. Chemical structure of Rolipram, a Autophagy inhibitor (SIH-401). CAS # 61413-54-5 . Molecular Formula: C16H21NO3.
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Warning information
Non-hazardous
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Country of production
Canada
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Total weight kg
0.25
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Net weight g
0.01
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Additional description
Tissue, pathway, proteinase, peptidase, protease ,acrosin, lipoprotein, activator, caspase, trypsin, papain, esterase inhibitors are proteins or receptor ligands or receptor antagonists that bind to an enzyme receptor and decreases its activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. Not all receptor antagonist that bind to enzymes are inhibitors; enzyme activator ligands or agonists bind to enzymes and increase their enzymatic activity, while enzyme substrates bind and are converted to products in the normal catalytic cycle of the enzyme.
