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1400W 2HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
1400W 2HCl图片
CAS NO:214358-33-5
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 250.17
Formula C10H15N3.2HCl
CAS No.214358-33-5 (HCl);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:35 mg/mL (139.9 mM)
Water:35 mg/mL (139.9 mM)
Ethanol:35 mg/mL (139.9 mM)
Solubility (In vivo)CC(NCC1=CC=CC(CN)=C1)=N.[H]Cl.[H]Cl
Synonyms1400W HCl; 1400-W hydrochloride; 1400 W HCl
实验参考方法
In Vitro

In vitro activity: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.


Kinase Assay: 1400W is a slow, tight binding, potent, and highly selective inhibitor of inducible nitric-oxide synthase (iNOS) with Ki values of 7 nM. The slow onset of inhibition by 1400W showed saturation kinetics with a maximal rate constant of 0.028 s-1 and a binding constant of 2.0 microM. Inhibition was dependent on the cofactor NADPH. L-Arginine was a competitive inhibitor of 1400W binding with a Ks value of 3.0 microM. Inhibited enzyme did not recover activity after 2 h. Thus, 1400W was either an irreversible inhibitor or an extremely slowly reversible inhibitor of human iNOS with a Kd value



Cell Assay: 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.

In Vivo1400W 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%);Treatment with 1400W can reduce the rate of growth of solid tumors in mice;
Animal model Rats
Formulation & Dosage isotonic saline; 0.1-10 mg/kg; s.c.
References J Biol Chem. 1997 Feb 21;272(8):4959-63;Cancer Res. 1997 Aug 1;57(15):3300-4.;