2016年6月12日星期日

(R)-(-)-Rolipram|cas 85416-75-7|DC Chemicals

(R)-(-)-Rolipram|cas 85416-75-7|DC Chemicals

(R)-(-)-Rolipram is a potent and cAMP-specific PDE4 inhibitor with  IC50 of 0.22 uM;  2.5-fold more potent than (+)-rolipram (IC50= 2.58 uM) in inhibiting membrane-bound PDE 4.

IC50 value:

Target: PDE4

in vitro: In intact eosinophils, (-)-rolipram (EC50 = 0.19 +/- 0.02 microM) was 10-fold more potent than (+)-rolipram (EC50 = 1.87 +/- 0.09 microM) in enhancing isoprenaline (10 microM)-stimulated cyclic AMP accumulation.

Product Name: (R)-(-)-Rolipram|Cat No: DC9584|Cas: 85416-75-7|Molecule Formular: C16H21NO3|Molecule Weight: 275.3428|Other names: (R)-(-)-Rolipram

(R)-(-)-Rolipram is a potent and cAMP-specific PDE4 inhibitor with  IC50 of 0.22 uM;  2.5-fold more potent than (+)-rolipram (IC50= 2.58 uM) in inhibiting membrane-bound PDE 4.
in vitro: In intact eosinophils, (-)-rolipram (EC50 = 0.19 +/- 0.02 microM) was 10-fold more potent than (+)-rolipram (EC50 = 1.87 +/- 0.09 microM) in enhancing isoprenaline (10 microM)-stimulated cyclic AMP accumulation. Rolipram was a relatively weak inhibitor of partially purified pig aortic PDE IV and only slight stereospecificity was exhibited [IC50 (-)-rolipram = 1.47 +/- 0.09 microM; IC50 (+)-rolipram = 2.73 +/- 0.38 microM]. The IC50 of rolipram (racemate) of these two fractions was 492 and 79 nM, respectively. The R-(-)-enantiomer of rolipram inhibited the cAMP-phosphodiesterase activity in the latter fraction 10 times more than did S-(+)-rolipram, and the inhibition of the former fraction was less stereospecific.

For research only, not for human use!

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