(R)-Lisofylline_product_DataBase

Bioactivity	(R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 µM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research[1][2].
Target	IC50: 0.6 µM (Lysophosphatidic acid acyltransferase)STAT4
Invitro	(R)-Lisofylline blocks IL-12-driven Th1 differentiation and T cell proliferation in vitro, yet has no effect on IL-12 secretion from APCs ex vivo or in vitro[3].
In Vivo	(R)-Lisofylline reduces the impairment of insulin secretion induced by IL-1β in cultured rat islet cells, suppresses IFN-γ production, the onset of diabetes, and macrophage infiltration into islets from NOD mice, as well as Lisofylline improves insulin response and lowers glucose levels in Streptozotocin-treated rats after the oral glucose tolerance test[1].(R)-Lisofylline prevents β cell dysfunction in NOD mice by inhibition of STAT4 phosphorylation which interrupts IL-12 signaling. (R)-Lisofylline ameliorates experimental allergic encephalomyelitis in mice[1]. (R)-Lisofylline also improves survival in mice injected with a lethal dose of LPS and ameliorates sepsis-induced lung injury in minipigs. In rats given IL-1 intratracheally (R)-Lisofylline pretreatment reduces lung leak but does not decrease neutrophil accumulation in lungs[1]. (R)-Lisofylline also suppresses release of TNF-α in vivo in mice and ex vivo in human blood stimulated with endotoxin derived from Salmonella or Escherichia coli[1].
Name	(R)-Lisofylline
CAS	100324-81-0
Formula	C13H20N4O3
Molar Mass	280.32
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	-20°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Reference	[1]. Elżbieta Wyska, et al. Physiologically Based Modeling of Lisofylline Pharmacokinetics Following Intravenous Administration in Mice. Eur J Drug Metab Pharmacokinet. 2016 Aug;41(4):403-12. [2]. B M Hybertson, et al. Lisofylline Prevents Leak, but Not Neutrophil Accumulation, in Lungs of Rats Given IL-1 Intratracheally. J Appl Physiol (1985). 1997 Jan;82(1):226-32. [3]. J J Bright, et al. Prevention of Experimental Allergic Encephalomyelitis via Inhibition of IL-12 Signaling and IL-12-mediated Th1 Differentiation: An Effect of the Novel Anti-Inflammatory Drug Lisofylline. J Immunol. 1998 Dec 15;161(12):7015-22.

PeptideDB

(R)-Lisofylline

CAS: 100324-81-0 F: C13H20N4O3 W: 280.32