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Submit Review1400W dihydrochloride
Description: Potent, highly selective iNOS inhibitor
Chemical Name: N-[[3-(Aminomethyl)phenyl]methyl]-ethanimidamide dihydrochloride
Purity: ≥99% (HPLC)
Biological Activity for 1400W dihydrochloride
1400W dihydrochloride is a slow, tight binding, potent and highly selective inhibitor of inducible nitric oxide synthase (Kd = 7 nM). Selective over nNOS and eNOS (Ki values are 2 and 50 μM respectively). Cell-permeable and active in vivo. Neuroprotective in epilepsy models and has analgesic effects in models of mechanical and heat hypersensitivity.
Technical Data for 1400W dihydrochloride
| M. Wt | 250.17 |
| Formula | C10H15N3.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 214358-33-5 |
| PubChem ID | 2733515 |
| InChI Key | WDJHSQZCZGPGAA-UHFFFAOYSA-N |
| Smiles | Cl.Cl.CC(=N)NCC1=CC=CC(CN)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for 1400W dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 25.02 | 100 |
Preparing Stock Solutions for 1400W dihydrochloride
The following data is based on the product molecular weight 250.17. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 4 mL | 19.99 mL | 39.97 mL |
| 5 mM | 0.8 mL | 4 mL | 7.99 mL |
| 10 mM | 0.4 mL | 2 mL | 4 mL |
| 50 mM | 0.08 mL | 0.4 mL | 0.8 mL |
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Product Datasheets for 1400W dihydrochloride
References for 1400W dihydrochloride
References are publications that support the biological activity of the product.
Garvey et al (1997) 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo. J.Biol.Chem. 272 4959 PMID: 9030556
Parmentier et al (1999) Selective inhibition of inducible nitric oxide synthase prevents ischaemic brain injury. Br.J.Pharmacol. 127 546 PMID: 10385257
Thomsen et al (1997) Selective inhibition of inducible nitric oxide inhibits tumor growth in vivo: studies with 1400W, a novel inhibitor. Cancer Res. 57 3300 PMID: 9242464
Staunton et al (2018) Inducible nitric oxide synthase inhibition by 1400W limits pain hypersensitivity in a neuropathic pain rat model. Exp.Physiol 103 535 PMID: 29441689
Putra et al (2020) Inducible nitric oxide synthase inhibitor, 1400W, mitigates DFP-induced long-term neurotoxicity in the rat model. Neurobiol.Dis. 133 104443 PMID: 30940499
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Keywords: 1400W dihydrochloride, 1400W dihydrochloride supplier, Potent, selective, iNOS, inhibitors, inhibits, Nitric, Oxide, Signaling, Signalling, Inducible, NO, Synthases, 1415, Tocris Bioscience
9 Citations for 1400W dihydrochloride
Citations are publications that use Tocris products. Selected citations for 1400W dihydrochloride include:
Gross et al (2013) Roles of endothelial nitric oxide synthase (eNOS) and mitochondrial permeability transition pore (MPTP) in epoxyeicosatrienoic acid (EET)-induced cardioprotection against infarction in intact rat hearts. J Mol Cell Cardiol 59 20 PMID: 23419451
Tsuda et al (2009) Mechanisms underlying fibronectin-induced up-regulation of P2X4R expression in microglia: distinct roles of PI3K-Akt and MEK-ERK signalling pathways. J Cell Mol Med 13 3251 PMID: 19298529
Kuen et al (2017) Pancreatic cancer cell/fibroblast co-culture induces M2 like macrophages that influence therapeutic response in a 3D model. PLoS One 12 e0182039 PMID: 28750018
Staunton et al (2018) Inducible nitric oxide synthase inhibition by 1400W limits pain hypersensitivity in a neuropathic pain rat model Exp Physiol 103 535 PMID: 29441689
Clark et al (2015) Selective activation of microglia facilitates synaptic strength. RNA 35 4552 PMID: 25788673
Gresa-Arribas et al (2012) Modelling neuroinflammation in vitro: a tool to test the potential neuroprotective effect of anti-inflammatory agents. PLoS One 7 e45227 PMID: 23028862
Müller et al (2018) Both Type I and Type II Interferons Can Activate Antitumor M1 Macrophages When Combined With TLR Stimulation. Front Immunol 9 2520 PMID: 30450098
Al-Shalmani et al (2011) Quercetin and its principal metabolites, but not myricetin, oppose lipopolysaccharide-induced hyporesponsiveness of the porcine isolated coronary artery. Br J Pharmacol 162 1485 PMID: 21375526
Ashrafpour et al (2004) Vasodilator effect and mechanism of action of vascular endothelial growth factor in skin vasculature. Am J Physiol Heart Circ Physiol 286 H946 PMID: 14644765
Do you know of a great paper that uses 1400W dihydrochloride from Tocris? Please let us know.
Reviews for 1400W dihydrochloride
Average Rating: 5 (Based on 3 Reviews.)
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Inhibition of iNOS by 1400W.
By
Anonymous on 04/03/2021
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: primary BMDM
Macrophages were treated with LPS (10 ng/mL) and IFN-y (20 ng/mL) for 24h in the presence of 1400W (100 uM)
1400W inhibits iNOS expression induced by LPS.
By
Anonymous on 05/16/2019
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: Macrophages
RAW macrophages were treated with 200 ng/ml LPS alone or after pre-treatment with 1 μM 1400W (30 min pre-incubation) for 8 h to follow iNOS expression using Western blot. LPS treatment elevated iNOS expression while 1400W pretreatment significantly blunted this effect.
iNOS inhibitor.
By
Anonymous on 07/28/2018
Assay Type: Ex Vivo
Species: Mouse
Used as iNOS inhibitor for organ bath experiments with rat and mouse aorta
Good solubility and stability