Rolipram Inhibitor CAS No. 61413-54-5

Cat. No.	Name	Size	Price
KI0735	Rolipram	10 mg	$234
	Rolipram	25 mg	$432
	Rolipram	50 mg	$592

Chemical Characteristic

Product Name	Rolipram
CAS No.	61413-54-5
Molecular Weight	275.34
Formula	C₁₆H₂₁NO₃
Chemical Structure

Biological activities

Rolipram is a potent and selective type IV-specific phosphodiesterase inhibitor. The IC50 of rolipram is 0.3 µM against phosphodiesterase 4 (PDE 4).^[1] Rolipram decreases the numbers of myelin basic protein-reactive IFN-γ and TNF-α mRNA-expressing blood mononuclear cells in multiple sclerosis. Rolipram also reduces numbers of AChR-reactive IFN-γ-, TNF-α-, and LT mRNA-positive cells in myasthenia gravis.^[2] Rolipram reveals pronounced ureteral relaxation with minimal circulatory effects.^[3] Rolipram suppresses inducible nitric oxide synthase at the mRNA level.^[4] Rolipram abrogates spinal cord injury-induced PDE4B1 and PDE4A5 production, PDE4A5 phosphorylation, MCP-1 expression and immune cell infiltration, while preventing post-injury reductions in IL-10.^[5] Rolipram pretreatment down-regulates both P- and E-selectin expression but has no effect on ICAM-1 and VCAM-1 expression.^[6] Rolipram directly inhibits TNF-钃?and IL-12 production following stimulation with IFN-γ and LPS.^[7] Rolipram (0.01閳?.0 mg/kg) attenuates the scopolamine-induced (0.5 mg/kg) increase in the total number of errors in dose- and time-dependent manners.^[8]

Protocols

In vivo: Rolipram is dissolved in PBS containing cremophor at a concentration of 10% (w/v).^[7]

References

[1] Dal Piaz V, et al. Phosphodiesterase 4 inhibitors, structurally unrelated to rolipram, as promising agents for the treatment of asthma and other pathologies. Eur J Med Chem. 2000, 35(5): 463-480. 閵嗏偓閵嗏偓 [2] Navikas V, et al. The phosphodiesterase i.v. inhibitor rolipram in vitro reduces the numbers of MBP-reactive IFN-gamma and TNF-alpha mRNA expressing blood mononuclear cells in patients with multiple sclerosis. Clin Neuropharmacol. 1998, 21(4): 236-244. 閵嗏偓閵嗏偓 [3] Becker AJ, et al. The effect of the specific phosphodiesterase-IV-inhibitor rolipram on the ureteral peristalsis of the rabbit in vitro and in vivo. J Urol. 1998, 160(3 Pt 1): 920-925. 閵嗏偓閵嗏偓 [4] Beshay E, et al. The phosphodiesterase inhibitors pentoxifylline and rolipram suppress macrophage activation and nitric oxide production in vitro and in vivo. Clin Immunol. 2001, 98(2): 272-279. 閵嗏偓閵嗏偓 [5] Schaal SM et al. The therapeutic profile of rolipram, PDE target and mechanism of action as a neuroprotectant following spinal cord injury. PLoS One. 2012, 7(9): e43634. 閵嗏偓閵嗏偓 [6] Sanz MJ, et al. Rolipram inhibits leukocyte-endothelial cell interactions in vivo through P- and E-selectin downregulation. Br J Pharmacol. 2002, 135(8): 1872-1881. 閵嗏偓閵嗏偓 [7] Ross SE, et al. Suppression of TNF-alpha expression, inhibition of Th1 activity, and amelioration of collagen-induced arthritis by rolipram. J Immunol. 1997, 159(12): 6253-6259. 閵嗏偓閵嗏偓 [8] Zhang HT, et al.Effects of rolipram on scopolamine-induced impairment of working and reference memory in the radial-arm maze tests in rats. Psychopharmacology (Berl). 2000, 150(3): 311-316. 閵嗏偓閵嗏偓

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