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1400W dihydrochlorideINOS inhibitor,potent and highly selective

1400W dihydrochloride

Catalog No. BCC7057
Size Price Stock
10mg $80.00 In stock
50mg $335.00 In stock
100mg $585.00 In stock
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Quality Control of 1400W dihydrochloride

Chemical structure

1400W dihydrochloride

Biological Activity of 1400W dihydrochloride

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.

1400W dihydrochloride Dilution Calculator

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Chemical Properties of 1400W dihydrochloride

Cas No. 214358-33-5 SDF Download SDF
Chemical Name N-[[3-(Aminomethyl)phenyl]methyl]-ethanimidamide dihydrochloride
SMILES CC(=NCC1=CC(=CC=C1)CN)N.Cl.Cl
Standard InChIKey FFSSUWWXUDLVQZ-UHFFFAOYSA-O
Standard InChI InChI=1S/C10H16N3/c1-8(12)13-7-10-4-2-3-9(5-10)6-11/h2-5,13H,6-7,11-12H2,1H3/q+1/p+1
Formula C10H15N3.2HCl M.Wt 250.17
Solubility Soluble to 100 mM in water
Storage Desiccate at RT
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other courier with RT , or blue ice upon request.

Preparing Stock Solutions of 1400W dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.9973 mL 19.9864 mL 39.9728 mL 79.9456 mL 99.932 mL
5 mM 0.7995 mL 3.9973 mL 7.9946 mL 15.9891 mL 19.9864 mL
10 mM 0.3997 mL 1.9986 mL 3.9973 mL 7.9946 mL 9.9932 mL
50 mM 0.0799 mL 0.3997 mL 0.7995 mL 1.5989 mL 1.9986 mL
100 mM 0.04 mL 0.1999 mL 0.3997 mL 0.7995 mL 0.9993 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

Background on 1400W dihydrochloride

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.

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