(R)-Lisofylline

CAS No. 100324-81-0

(R)-Lisofylline( —— )

Catalog No. M27451 CAS No. 100324-81-0

(R)-Lisofylline is an inhibitor of lysophosphatidic acid acyltransferase (IC50 = 0.6 μM).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    (R)-Lisofylline
  • Note
    Research use only, not for human use.
  • Brief Description
    (R)-Lisofylline is an inhibitor of lysophosphatidic acid acyltransferase (IC50 = 0.6 μM).
  • Description
    (R)-Lisofylline is an inhibitor of lysophosphatidic acid acyltransferase (IC50 = 0.6 μM). (R)-Lisofylline interrupts IL-12 signaling-mediated STAT4 activation and can be used in studies about the treatment of type 1 diabetes and autoimmune disorders.(In Vitro):(R)-Lisofylline blocks IL-12-driven T cell proliferation and Th1 differentiation yet has no effect on IL-12 secretion.(In Vivo):In NOD mice, (R)-Lisofylline prevents β cell dysfunction by inhibition of STAT4 phosphorylation and ameliorates experimental allergic encephalomyelitis. (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. (R)-Lisofylline improves insulin response and lowers glucose levels in Streptozotocin-treated rats after the oral glucose tolerance test. In rats given IL-1 intratracheally (R)-Lisofylline pretreatment reduces lung leak but does not decrease neutrophil accumulation in lungs. (R)-Lisofylline improves survival in mice injected with a lethal dose of LPS and ameliorates sepsis-induced lung injury in minipigs.
  • In Vitro
    (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.
  • 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.(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. (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. (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.
  • Synonyms
    ——
  • Pathway
    JAK/STAT Signaling
  • Target
    STAT
  • Recptor
    Cereblon|PEGs
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    100324-81-0
  • Formula Weight
    280.32
  • Molecular Formula
    C13H20N4O3
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 100 mg/mL (356.74 mM)
  • SMILES
    O=C1C2=C(N(C)C(=O)N1CCCC[C@@H](C)O)N=CN2C
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression. J Med Chem. 2019 Jan 24;62(2):448-466.
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