R-(-)-RolipramA PDE IV inhibitor and anti-inflammatory agent

R-(-)-Rolipram (CAS 85416-75-7)

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Application: A PDE IV inhibitor and anti-inflammatory agent
CAS Number: 85416-75-7
Purity: 98%
Molecular Weight: 275.34
Molecular Formula: C16H21NO3
* Refer to Certificate of Analysis for lot specific data (including water content).
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R-(-)-Rolipram is the R-entantiomer of rolipram. This compound has been shown to strongly inhibit the catalytic activities of PDE4 (phosphodiesterase 4), which is selective for cAMP, an important secondary messenger molecule in signal transduction. Experiments have revealed that high-affinity binding sites require residues within the catalytic domains and residues flanking the N-/C-terminal to the catalytic region of amino acids. Other studies suggest that the deactivation of PDE4 has been reported to affect other cellular functions.


References

1. Torphy, T.J., et al. 1992. J. Biol. Chem. 267: 1798-1804. PMID: 1309798
2. Underwood, D.C., et al. 1993. J. Pharmacol. Exp. Ther. 266: 306-313. PMID: 8392555
3. Grous, M. and Barnette, M. 1994. Br. J. Pharmacol. 111: 259-263. PMID: 7516803
4. Rocque, W.J., et al. 1997. Protein Expr. Purif. 9: 191-202. PMID: 9056484
5. Ohsawa, F., et al. 1998. Jpn. J. Pharmacol. 77: 147-154. PMID: 9681571

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml warm), and ethanol (25 mg/ml).
Storage :
Store at 4° C
Melting Point :
132.2° C
Boiling Point :
472.74° C at 760 mmHg (Predicted)
Density :
1.16 g/cm3 (Predicted)
Refractive Index :
n20D 1.55 (Predicted)
IC50 :
antigen-induced contraction of guinea-pig colonic smooth muscle: EC5050 = 0.1 µM; Phosphodiesterase 4A: IC50 = 162 nM (human); Phosphodiesterase 4B: IC50 = 231 nM (human); Phosphodiesterase 4D: IC50 = 622 nM (human)
Ki Data :
PDE IV: Ki= 0.6 µM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
5092
MDL Number :
MFCD03093861
SMILES :
COC1=C(C=C(C=C1)C2CC(=O)NC2)OC3CCCC3

Download SDS (MSDS)

Certificate of Analysis

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