1400W dihydrochloride是高效选择性的诱导型一氧化氮合成酶抑制剂(Ki:7 nM)。

1400 W is a highly effective and specific inhibitor of inducible NOS2 (iNOS).

1400W is either an irreversible inhibitor or an extremely slowly reversible inhibitor of human iNOS. Inhibition of human iNOS by 1400W is time-dependent. 1400W is competitive with L-arginine. 1400W is not a substrate for iNOS[1].

1400W selectively prevents microvasculature injury in rats. 1400W is greater than 50-fold more potent against iNOS than eNOS in a rat model of endotoxin-induced vascular injury. Moreover, 1400W also dose-dependently reduces LPS-induced vascular leakage associated with iNOS induction in the colon, lung, liver, kidney, and heart. The maximal protection is close to 100% for all organs except the kidney (kidney:54%)[1]. 1400W has an ameliorative effect on both oxidative and nitrosative stress in the kidneys against renal I/R injury in rats[2]. Treatment with 1400W can reduce the rate of growth of solid tumors in mice[4].

RAW264.7 cells are treated with LPS/IFNγ for 16 h and GAPDH-p300 binding is abolished by the iNOS inhibitor 1400W (100 μM). Cell lysates are immunoprecipitated with an anti-p300 antibody and the immunoprecipitates are analysed by western blotting with an anti-GAPDH antibody. (Only for Reference)

214358-33-5

C10H17Cl2N3

250.17

1400W 2HCl;N-(3-(Aminomethyl)benzyl)acetamidine

H2O:139.9 mM
DMSO:139.9 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years