product name Rolipram
Description: Rolipram (also known as ZK-62711, SB 95952) is a potent PDE4 inhibitor and an anti-inflammatory agent. Rolipram is the racemic mixture of R- and S-rolipram, it inhibits human monocyte. Rolipram inhibits human monocyte cyclic AMP-specific PDE4 with IC50 of 0.75 μM. It has potent anti-inflammatory and anti-depressant activity in the central nervous system, and the S-(+)-Rolipram is less potent than its R enantiomer.
References: Trends Pharmacol Sci. 1997 May;18(5):164-71; Br J Pharmacol. 1996 Jun;118(3):649-58; J Pharmacol Exp Ther. 1993 Jul;266(1):306-13.
275.34
Formula
C16H21NO3
CAS No.
61413-54-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 55 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 55 mg/mL (199.8 mM)
Solubility (In vivo)
30% PEG400+0.5% Tween80+5% propylene glycol: 10 mg/L
Synonyms
ZK-62711, SB 95952
other peoduct :
| In Vitro |
In vitro activity: S-(+)-Rolipram suppresses LPS-induced TNFα expression from human monocyte through inhibiting PDE4 with IC50 about 2 μM. 1 μM S-(+)-Rolipram significantly antagonizes ovalbumin (OA) induced concentration-related contractions of tracheal rings which are isolated from OA-sensitized guinea pigs. S-(+)-Rolipram inhibits PDE4 activity in a CHO-K1 cell line which stably expresses a recombinant full length human PDE-4a with IC50 at 450 nM. Treatment of the human glioma cell line A-172 with Rolipram (including both R- and S-enantiomers of Rolipram) results in increased expression of the cell cycle inhibitors p21 and p27, and decreased activity of cdk2, a cyclindependent kinase essential for cell cycle progression. As a result, the proliferation of A-172 cells is inhibited, with induction of a G1 block. Eventually, Rolipram-treated A-172 cells undergo differentiation, which is followed by apoptotic cell death. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In anesthetized, ventilated OA-sensitive guinea pigs, S-(+)-Rolipram reduces OA-induced bronchoconstriction with ID50 values of approximately 0.25 mg/kg i.v. Histamine- and leukotriene D4-induced bronchoconstriction are not affected by doses of S-(+)-Rolipram which abolishes the response to OA. Higher doses (3-10 mg/kg) reduce histamine-, but not the leukotriene D4-induced bronchoconstriction. In conscious OA-sensitive guinea pigs, intragastric pretreatment with S-(+)-Rolipram dose-dependently reduces both the OA-induced decreases in specific conductance as well as the corresponding pulmonary eosinophil influx as assessed by both bronchoalveolar lavage and histological evaluation. |
| Animal model | Male Hartley guinea pigs |
| Formulation & Dosage | Dissolved in 100% PEG at an appropriate concentration; 1 mL/kg; i.v. injection |
| References | Trends Pharmacol Sci. 1997 May;18(5):164-71; Br J Pharmacol. 1996 Jun;118(3):649-58; J Pharmacol Exp Ther. 1993 Jul;266(1):306-13. |
