GW274150

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GW274150 是一种有效且高度选择性的 iNOS 抑制剂，IC50 为 1.4 uM，

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.

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.

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.

GW-274150 | GW 274150

Immunology/Inflammation

NOS

NOS

Inflammation/Immunology

Rheumatoid Arthritis

210354-22-6

219.3045

C8H17N3O2S

>98% (HPLC)

H2O: ≥ 62 mg/mL

CC(=N)NCCSCC[C@@H](C(=O)O)N

L-Homocysteine, S-[2-[(1-iminoethyl)amino]ethyl]-

(-20℃)

With Ice Pack

≥ 2 years