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Purity: ≥98%
1400W (1400-W) is a slow, tight binding, potent, and highly selective inhibitor of inducible nitric-oxide synthase (iNOS) with Ki values of 7 nM. The slow onset of inhibition by 1400W showed saturation kinetics with a maximal rate constant of 0.028 s-1 and a binding constant of 2.0 microM. Inhibition was dependent on the cofactor NADPH. L-Arginine was a competitive inhibitor of 1400W binding with a Ks value of 3.0 microM. Inhibited enzyme did not recover activity after 2 h. Thus, 1400W was either an irreversible inhibitor or an extremely slowly reversible inhibitor of human iNOS with a Kd value
| ln Vitro |
1400W is a human inducible nitric-oxide synthase (iNOS) inhibitor that binds slowly and tightly. Saturation kinetics are evident in the gradual onset of inhibition by 1400W, with a maximal rate constant of 0.028 s-1 and a binding constant of 2.0 μM. NADPH is required as a cofactor for inhibition. For iNOS compared to eNOS, 1400W is at least 5000 times more selective. By comparison, the inhibition of endothelial NOS (eNOS) and human neuronal NOS (Ki values of 2 μM and 50 μM, respectively], is competitive with L-arginine, quickly reversible, and relatively weaker[1]. Without influencing nNOS or eNOS, 1400W treatment inhibits the expression of iNOS. In the cerebral cortex, 1400W also inhibits the production of NO, 3-NT, and MDA and stops the death of neural cells[2].
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| ln Vivo |
In rats exposed to LPS-induced iNOS, 1400W potently (ED50=0.3 mg/kg) decreases the delayed vascular injury, but when administered in conjunction with LPS, it does not worsen acute vascular leakage[1]. Every experimental group's NOx levels are reduced by the administration of 1400W. Furthermore, the late post-hypoxia period (48 hours and 5 days) is marked by lipid peroxidation, the proportion of apoptotic cells, and nitrated protein expression[3].
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| 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 |
| Molecular Formula |
C10H15N3.2HCL
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| Molecular Weight |
250.17
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| CAS # |
214358-33-5
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| Related CAS # |
180001-34-7;214358-33-5 (HCl);
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| SMILES |
Cl[H].Cl[H].N(=C(/C([H])([H])[H])\N([H])[H])/C([H])([H])C1=C([H])C([H])=C([H])C(C([H])([H])N([H])[H])=C1[H]
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2 mg/mL (7.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (399.73 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9973 mL | 19.9864 mL | 39.9728 mL | |
| 5 mM | 0.7995 mL | 3.9973 mL | 7.9946 mL | |
| 10 mM | 0.3997 mL | 1.9986 mL | 3.9973 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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