Description
1400W dihydrochloride is a potent and selective inhibitor of human inducible NO synthase with Ki values of 7 nM.
Product information
CAS Number: 214358-33-5
Molecular Weight: 250.17
Formula: C10H17Cl2N3
Chemical Name: (E)-N'-{[3-(aminomethyl)phenyl]methyl}ethanimidamide dihydrochloride
Smiles: Cl.Cl.C/C(/N)=N\CC1C=C(CN)C=CC=1
InChiKey: WDJHSQZCZGPGAA-UHFFFAOYSA-N
InChi: InChI=1S/C10H15N3.2ClH/c1-8(12)13-7-10-4-2-3-9(5-10)6-11;;/h2-5H,6-7,11H2,1H3,(H2,12,13);2*1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 20 mg/mL (79.95 mM; Need ultrasonic). H2O : 100 mg/mL (399.73 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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. 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.
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. 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).
Products are for research use only. Not for human use.
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