Home Immunology & Inflammation NOS inhibitor 1400W 2HCl

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1400W 2HCl NOS inhibitor

Cat.No.S8337

1400W (N-(3-(Aminomethyl)benzyl)acetamidine) is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase(iNOS).
1400W 2HCl NOS inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 250.17

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Quality Control

Batch: Purity: 99.89%
99.89

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50=0.2μM 23232148
RAW264.7 Antiinflammatory assay 20 hrs Antiinflammatory activity against LPS-stimulated mouse RAW264.7 cells assessed as nitrite accumulation after 20 hrs by fluorimetry, IC50=0.3μM 11678654
RAW264.7 Function assay Inhibition of LPS-induced nitric oxide generation in mouse RAW264.7 cells pretreated 1 hr before LPS challenge by Griess method, IC50=1.5μM 19278854
N9 Function assay Inhibitory effect of compound on the accumulation of NO2 in the culture media of N9 cells in response to LPS/IFN-gamma, IC50=2.2μM 15013012
RAW264.7 Antiinflammatory assay Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of nitric oxide production pretreated 1 hr before LPS challenge, IC50=2.3μM 12662101
RAW264.7 Function assay Inhibition of LPS-induced nitric oxide accumulation in mouse RAW264.7 cells, IC50=2.7μM 19699097
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite accumulation after 24 hrs, IC50=2.9μM 15568764
RAW264.7 Antiinflammatory assay 24 hrs Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on NO production pretreated 1 hr before LPS challenge measured after 24 hrs, IC50=3.1μM 11908984
N9 Antiinflammatory assay Antiinflammatory activity in LPS/IFN-gamma-stimulated mouse N9 cells assessed as inhibition of nitric oxide production pretreated 1 hr before LPS/IFNgamma challenge, IC50=3.6μM 12662101
RAW264.7 Function assay Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells, IC50=3.78μM 17988874
RAW 264 Function assay 24 hrs Inhibition of 1ug/ml LPS-stimulated nitirc oxide accumulation in RAW 264 cells after 24 hrs, IC50=5.2μM 17320246
RAW264.7 Function assay Inhibitory effect of compound on the accumulation of NO2 in the culture media of RAW 264.7 cells in response to LPS, IC50=6.1μM 15013012
N9 Antiinflammatory assay 24 hrs Antiinflammatory activity against mouse N9 cells assessed as inhibition of LPS/IFN-gamma-induced nitrite accumulation after 24 hrs, IC50=6.3μM 15568764
RAW264.7 Cytotoxicity assay 24 hrs Cytotoxicity against mouse RAW264.7 cells assessed as cell viability after 24 hrs by MTS assay, IC50=47.47μM 23232148
RAW264.7 Antiinflammatory assay 50 uM 24 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 50 uM treated 30 mins before LPS challenge measured after 24 hrs by Griess method 20447741
RAW264.7 Antiinflammatory assay 0.5 to 2 uM 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced COX-2 expression at 0.5 to 2 uM incubated for 2 hrs prior to LPS challenge measured after 24 hrs by Western blot analysis 23232148
RAW264.7 Antiinflammatory assay 2 uM 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as downregulation of LPS-induced iNOS mRNA expression at 2 uM incubated for 2 hrs prior to LPS challenge measured after 9 hrs by RT-PCR analysis 23232148
RAW264.7 Antiinflammatory assay 0.5 to 2 uM 2 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS expression at 0.5 to 2 uM incubated for 2 hrs prior to LPS challenge measured after 24 hrs by Western blot analysis 23232148
RAW264.7 Function assay 4 uM Inhibition iNOS mRNA expression levels in LPS-induced mouse RAW264.7 cells at 4 uM by RT-PCR analysis 27542306
RAW264.7 Function assay 4 uM Inhibition iNOS protein expression levels in LPS-induced mouse RAW264.7 cells at 4 uM by Western blot analysis 27542306
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Solubility

In vitro
Batch:

DMSO : 35 mg/mL (139.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 35 mg/mL

Ethanol : 35 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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g
μL

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%
% Tween 80
% ddH2O
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 250.17 Formula

C10H15N3.2HCl

 Storage (From the date of receipt)
CAS No. 214358-33-5 Download SDF Storage of Stock Solutions

Synonyms N-(3-(Aminomethyl)benzyl)acetamidine Smiles CC(=NCC1=CC=CC(=C1)CN)N.Cl.Cl

Mechanism of Action

Targets/IC50/Ki
iNOS
(Cell-free assay)
<7 nM(Kd)
nNOS
(Cell-free assay)
2 μM(Ki)
eNOS
(Cell-free assay)
50 μM(Ki)
In vitro
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.
In vivo
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%). 1400W has an ameliorative effect on both oxidative and nitrosative stress in the kidneys against renal I/R injury in rats. Treatment with 1400W can reduce the rate of growth of solid tumors in mice.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9242464/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00845169 Completed
Endothelial Dysfunction
University of Edinburgh|NHS Lothian|Umeå University
 April 2012 Not Applicable

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