CAS 214358-33-5|1400W dihydrochloride
| Common Name | 1400W dihydrochloride | ||
|---|---|---|---|
| CAS Number | 214358-33-5 | Molecular Weight | 250.168 |
| Density | / | Boiling Point | 329ºC at 760 mmHg |
| Molecular Formula | C10H17Cl2N3 | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | 152.7ºC |
Names
| Name | 1400W (hydrochloride) |
|---|---|
| Synonym | More Synonyms |
1400W dihydrochloride BiologicalActivity
| Description | 1400W dihydrochloride is a potent and selective inhibitor of human inducible NO synthase with Ki values of 7 nM. |
|---|---|
| Related Catalog | Signaling Pathways >>Immunology/Inflammation >>NO SynthaseResearch Areas >>Cardiovascular DiseaseResearch Areas >>Inflammation/Immunology |
| 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 | [1]. Garvey EP, et al. 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo. J Biol Chem. 1997 Feb 21;272(8):4959-63. [2]. Shi Q, et al. 1400W ameliorates acute hypobaric hypoxia/reoxygenation-induced cognitive deficits by suppressing the induction of inducible nitric oxide synthase in rat cerebral cortex microglia. Behav Brain Res. 2017 Feb 15;319:188-199. [3]. Rus A, et al. Inducible NOS inhibitor 1400W reduces hypoxia/re-oxygenation injury in rat lung. Redox Rep. 2010;15(4):169-78. |
Chemical & Physical Properties
| Boiling Point | 329ºC at 760 mmHg |
|---|---|
| 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 |
| InChIKey | WDJHSQZCZGPGAA-UHFFFAOYSA-N |
| SMILES | CC(N)=NCc1cccc(CN)c1.Cl.Cl |
| Storage condition | -20℃ |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
Articles4
More Articles| NOS1-dependent negative feedback regulation of the epithelial sodium channel in the collecting duct. Am. J. Physiol. Renal Physiol. 308(3) , F244-51, (2015) With an increase in urine flow there is a significant increase in shear stress against the renal epithelium including the inner medullary collecting duct, resulting in an increase in nitric oxide (NO)... | |
| Gardenamide A Protects RGC-5 Cells from H₂O₂-Induced Oxidative Stress Insults by Activating PI3K/Akt/eNOS Signaling Pathway. Int. J. Mol. Sci. 16 , 22350-67, (2015) Gardenamide A (GA) protects the rat retinal ganglion (RGC-5) cells against cell apoptosis induced by H₂O₂. The protective effect of GA was completely abrogated by the specific phosphoinositide 3-kinas... | |
| Selective inhibition of inducible nitric oxide synthase inhibits tumor growth in vivo: studies with 1400W, a novel inhibitor. Cancer Res. 57 , 3300, (1997) We have investigated the effect of N-(3-(aminomethyl)benzyl)acetamidine (1400W), a novel and highly selective inhibitor for inducible NOS (iNOS), on in vivo growth of solid tumors expressing iNOS. For... |
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) |
