A selective inhibitor of PDE4, Rolipram, inhibits immunopurified PDE4B and PDE4D activity with IC50 of 130 nM and 240 nM, respectively. It has anti-inflammatory activity.

 

Brand: BCM

 

Target: HIV Protease; Antibacterial; PDE

Signaling Pathways: Metabolism; Microbiology/Virology; Proteases/Proteasome

 

In Vitro: The PDE4 selective inhibitor, Rolipram, inhibits immunopurified PDE4B and PDE4D activities similarly, with IC50s of approx. 130 nM and 240 nM respectively. In contrast, Rolipram inhibits immunopurified PDE4A activity with a dramatically lower IC50 of around 3 nM. Rolipram increases phosphorylation of cAMP-response-element-binding protein (CREB) in U937 cells in a dose-dependent fashion, which means that both high affinity (IC50 approx. 1 nM) and low affinity (IC50 approx. 120 nM) components are presented. Rolipram dose-dependently inhibits the IFN-gamma-stimulated phosphorylation of p38 MAPK in a simple monotonic fashion with an IC50 of approx. 290 nM. Rolipram is a selective PDE4 inhibitor that inhibits all PDE4 isoforms A, B, C and D. Rolipram inhibits LPS-induced TNF production in a dose-dependent manner (IC50 25.9 nM), and maximal/submaximal inhibition is observed with 2 μM drug concentration in J774 cells.

 

Melting Point: 127-133 °C

 

Boiling Point: 418.29°C (rough estimate)

 

pKa: 16.02±0.40(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Ethanol. Insoluble in Water.

 

GHS: GHS07

 

Isomeric SMILES: COC1=C(C=C(C=C1)C2CC(=O)NC2)OC3CCCC3  

 

InChIKey: HJORMJIFDVBMOB-UHFFFAOYSA-N  

 

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)

 

Attribute
[Chem Name]	4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidin-2-one
[Synonym]	Rolipram; ZK-62711; SB 95952
[CAS No.]	61413-54-5
[EINECS]	262-771-1
[MDL No.]	MFCD00270906
[Formula]	C16H21NO3
[Molecular]	275.34
[Form]	White to off-white solid
[Storage]	Sealed in dry. Store in freezer, under -20°C

Goods Tag