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1400W dihydrochloride

Catalog No.GC13563

INOS inhibitor,potent and highly selective

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1400W dihydrochloride Chemical Structure

Cas No.: 214358-33-5

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10mg
$57.00
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50mg
$239.00
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100mg
$411.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment [1]:

Kinase assays

The oxidation of L-[14C]arginine was monitored by the conversion of L-[14C]arginine to L-[14C]citrulline. The enzyme was assayed at 37°C in 20 mM Hepes, pH 7.4, with 2.5 mM dithiothreitol, 125 μM NADPH, 10 μM tetrahydrobiopterin, 10 μM FAD, and 0.5-20 μM L-[14C]arginine (10,000 cpm). When eNOS or nNOS were assayed, calmodulin (10 μg/ml) and CaCl2 (2.5 mM) were included. When time courses were measured, bovine serum albumin (1 mg/ml) was included.

Animal experiment [1]:

Animal models

Rat model of endotoxin-induced microvascular injury

Dosage form

0.1-10 mg/kg, subcutaneous

Application

1400W was a potent inhibitor against iNOS in a rat model of endotoxin-induced vascular injury. When administered 3 h after endotoxin, 1400W completely suppressed leakage into the ileum. 1400W has an effect of endotoxin -induced vascular injury in the ileum.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Garvey EP, Oplinger JA, Furfine ES, 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, 272(8): 4959-4963.

Background

1400W dihydrochloride is a potent and selective inhibitor of inducible nitric oxide synthase with Kd value of 7 nM [1].

Inducible nitric oxide synthase (iNOS) is an enzyme catalyzing the production of nitric oxide (NO) and is involved in immune response. iNOS produces NO as an immune defense mechanism.

1400W dihydrochloride is an extremely slowly reversible and selective iNOS inhibitor [1]. 1400W inhibited iNOS with Kd value of 7 nM and rapidly reversibly inhibited human neuronal NOS (nNOS) and endothelial NOS (eNOS) with Ki values of 2 and 50 μM, respectively. L-arginine was a competitive inhibitor of 1400W with Ks value of 3.0 μM [1].

In an endotoxin-induced vascular injury rat model, 1400W exhibited 50-fold more potent selectivity against iNOS than eNOS [1]. In focal cerebral ischaemia rats, 1400W (20 mg/kg) inhibited neurological dysfunction and weight loss and significantly decreased ischaemic lesion volume by 31%. Also, 1400W reduced iNOS activity by 36% in the infarct [2]. In the EMT6 murine mammary adenocarcinoma, 1400W (10 or 12 mg/kg/h) significantly reduced tumor weight and inhibited iNOS activity [3].

References:
[1].  Garvey EP, Oplinger JA, Furfine ES, 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, 272(8): 4959-4963.
[2].  Thomsen LL, Scott JM, Topley P, et al. Selective inhibition of inducible nitric oxide synthase inhibits tumor growth in vivo: studies with 1400W, a novel inhibitor. Cancer Res, 1997, 57(15): 3300-3304.
[3].  Parmentier S, Böhme GA, Lerouet D, et al. Selective inhibition of inducible nitric oxide synthase prevents ischaemic brain injury. Br J Pharmacol, 1999, 127(2): 546-552.

Chemical Properties

Cas No. 214358-33-5 SDF
Chemical Name (E)-N'-(3-(aminomethyl)benzyl)acetimidamide dihydrochloride
Canonical SMILES NCC1=CC(C/N=C(C)/N)=CC=C1.Cl.Cl
Formula C10H15N3.2HCl M.Wt 250.17
Solubility ≥ 25mg/mL in DMSO Storage Desiccate at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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