Name | 1400W (hydrochloride) |
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Synonyms |
(1E)-N'-[3-(Aminomethyl)benzyl]ethanimidamide dihydrochloride
1400 W dihydrochloride MFCD03428622 Ethanimidamide, N'-[[3-(aminomethyl)phenyl]methyl]-, (1E)-, hydrochloride (1:2) 1400W dihydrochloride 1400W (Dihydrochloride) |
Description | 1400W dihydrochloride is a potent and selective inhibitor of human inducible NO synthase with Ki values of 7 nM. |
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Related Catalog | |
Target |
Ki: 7 nM (iNOS), 2 µM (nNOS), 50 µM (eNOS)[1] |
In Vitro | 1400W is a slow, tight binding inhibitor of human inducible nitric- oxide synthase (iNOS). The slow onset of inhibition by 1400W shows saturation kinetics with a maximal rate constant of 0.028 s-1 and a binding constant of 2.0 μM. Inhibition is dependent on the cofactor NADPH. 1400W is at least 5000-fold selective for iNOS versus eNOS. In contrast, inhibition of human neuronal NOS and endothelial NOS (eNOS) is relatively weaker, rapidly reversible, and competitive with L-arginine, with Ki values of 2 μM and 50 μM, respectively[1]. 1400W treatment inhibits iNOS expression without affecting nNOS or eNOS. 1400W also reduces NO, 3-NT and MDA production, and prevents neuronal cell apoptosis in cerebral cortex[2]. |
In Vivo | 1400W potently (ED50=0.3 mg/kg) reduces the delayed vascular injury in rats attributable to LPS-induced iNOS but fails to exacerbate acute vascular leakage when given concurrently with LPS[1]. Administration of 1400W lowers NOx levels in all the experimental groups. In addition, lipid peroxidation, the percentage of apoptotic cells, and nitrated protein expression fall in the late post-hypoxia period (48 h and 5 days)[3]. |
Animal Admin | Rats: The effects of 1400W on plasma leakage are assessed in rats by determining the leakage of [125I]human serum albumin from plasma into organs. 1400W (0.1-10 mg/kg, subcutaneous) is dissolved in isotonic saline and administered either concurrently with endotoxin or 3 h following LPS administration (E. coli LPS, 3 mg/kg intravenously). Plasma leakage is then assessed 1 or 5 h after delivery of 1400W[1]. |
References |
Boiling Point | 329ºC at 760 mmHg |
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Molecular Formula | C10H17Cl2N3 |
Molecular Weight | 250.168 |
Flash Point | 152.7ºC |
Exact Mass | 249.079956 |
PSA | 61.90000 |
LogP | 4.02700 |
Vapour Pressure | 0.000183mmHg at 25°C |
Storage condition | -20℃ |
Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
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RIDADR | NONH for all modes of transport |