GW274150

CAS No. 210354-22-6

GW274150( GW-274150 | GW 274150 )

Catalog No. M13344 CAS No. 210354-22-6

GW274150 is a potent and highly selective inhibitor of iNOS with IC50 of 1.4 uM,

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    GW274150
  • Note
    Research use only, not for human use.
  • Brief Description
    GW274150 is a potent and highly selective inhibitor of iNOS with IC50 of 1.4 uM,
  • Description
    GW274150 is a potent and highly selective inhibitor of iNOS with IC50 of 1.4 uM, displays >200 fold selectivity over eNOS and nNOS (IC50>100 uM); attenuates the degree of chronic inflammation and tissue damage associated with collagen-induced arthritis in mice; significantly reduces serum urea, serum creatinine, AST, and NAG, reduces experimental renal ischemia/reperfusion injury.Rheumatoid Arthritis Phase 2 Discontinued.
  • In Vitro
    GW274150 inhibits intracellular iNOS in J774 cells in a time-dependent manner, reaching IC50?values of 0.2 μM.GW274150?is >260-fold and 219-fold selective for iNOS against eNOS and nNOS in rat tissues, respectively. And it displays >100-fold and >80-fold for human iNOS against human eNOS and nNOS, respectively.
  • In Vivo
    GW274150 is a long-acting (5 h half‐life in rats) iNOS inhibitor and is able to inhibit LPS‐mediated increase in plasma NO2-,?NO3-?levels 14 h after single intraperitoneal dose (ED50=3 mg/kg).GW274150 (intraperitoneal?injection; 2.5, 5, and 10 mg/kg; before carrageenan injection) reduces the degree of lung injury induced by carrageenan in a dose-related fashion. Oedema formation and PMNs infiltration in the pleural cavity are also significantly attenuated in a dose‐related manner in rats.GW274150 (oral adminstration; 30 mg/kg; twice daily; 7 days) leads to significant neuroprotection, However, it displays a bell-shaped neuroprotective profile, being ineffective at high doses in 6-OHDA rat model of Parkinson disease (PD). Animal Model:SD-rat Dosage:2.5, 5 and 10 mg/kg; single dose Administration:Intraperitoneal?injection 5 min before carrageenan injection Result:Exerted a protective role in an acute model of inflammation, carrageenan-induced lung injury.
  • Synonyms
    GW-274150 | GW 274150
  • Pathway
    Immunology/Inflammation
  • Target
    NOS
  • Recptor
    NOS
  • Research Area
    Inflammation/Immunology
  • Indication
    Rheumatoid Arthritis

Chemical Information

  • CAS Number
    210354-22-6
  • Formula Weight
    219.3045
  • Molecular Formula
    C8H17N3O2S
  • Purity
    >98% (HPLC)
  • Solubility
    H2O: ≥ 62 mg/mL
  • SMILES
    CC(=N)NCCSCC[C@@H](C(=O)O)N
  • Chemical Name
    L-Homocysteine, S-[2-[(1-iminoethyl)amino]ethyl]-

Shipping & Storage Information

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

Reference

1. Young RJ, et al. Bioorg Med Chem Lett. 2000 Mar 20;10(6):597-600. 2. Cuzzocrea S, et al. Eur J Pharmacol. 2002 Oct 18;453(1):119-29. 3. McDonald MC, et al. J Physiol Pharmacol. 2002 Dec;53(4 Pt 1):555-69. 4. Chatterjee PK, et al. Kidney Int. 2003 Mar;63(3):853-65.
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