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1400W . dihydrochloride

iNOS inhibitor
 
ALX-270-073-M005 5 mg 59.00 USD
 
ALX-270-073-M025 25 mg 168.00 USD
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Replaces Prod. #: BML-CN268

A slow, tight binding and highly selective inhibitor of inducible nitric oxide synthase (iNOS/NOS II) in vitro and in vivo. Binds tightly to iNOS with a Kd of 7nM. In contrast, inhibition of nNOS and eNOS is weaker and rapidly reversible with Ki values of 2 and 50µM respectively. Inhibits tumor growth in vivo. Prevents circulatory failure but not organ injury induced by endotoxin. Displays protective effects in oxygen-deprived brain slices.

Product Specification

Formula:C10H15N3 . 2HCl
 
MW:177.3 . 73.0
 
Source:Synthetic.
 
CAS:214358-33-5
 
Purity:≥95% (TLC)
 
Identity:Determined by NMR.
 
Appearance:White to off-white powder.
 
Solubility:Soluble in water (up to 25mg/ml), methanol or DMSO.
 
Shipping:Ambient
 
Short Term Storage:-20°C
 
Long Term Storage:-20°C
 
Handling:Hygroscopic.
 
ALX-270-073
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ALX-270-073

Product Literature References

Chemically Bonding of Amantadine with Gardenamide A Enhances the Neuroprotective Effects against Corticosterone-Induced Insults in PC12 Cells: J. Zhao, et al.; Int. J. Mol. Sci. 16, 22795 (2015), Application(s): Cell Culture, Abstract; Full Text
Levosimendan inhibits interleukin-1β-induced apoptosis through activation of Akt and inhibition of inducible nitric oxide synthase in rat cardiac fibroblasts: M. Okada, et al.; Eur. J. Pharmacol. 769, 86 (2015), Application(s): Cell culture , Abstract;
Pretreatment with Relaxin Does Not Restore NO-Mediated Modulation of Calcium Signal in Coronary Endothelial Cells Isolated from Spontaneously Hypertensive Rats: S. Nistri, et al.; Molecules 20, 9524 (2015), Application(s): Cell Culture, Abstract; Full Text
Toll-like receptor 4 signaling confers cardiac protection against ischemic injury via inducible nitric oxide synthase- and soluble guanylate cyclase-dependent mechanisms: E. Wang, et al.; Anesthesiology 114, 603 (2010), Abstract; Full Text
Effects of 1400W, a potent selective inducible NOS inhibitor, on histamine- and leukotriene D4-induced relaxation of isolated guinea pig nasal mucosa: Y. Chiba, et al.; Nitric Oxide 15, 142 (2006), Abstract;
1400W, a potent selective inducible NOS inhibitor, improves histopathological outcome following traumatic brain injury in rats: M. Jafarian-Tehrani, et al.; Nitric Oxide 12, 61 (2005), Abstract;
Addition of nitric oxide donor S-nitroso-N-acetylcysteine to selective iNOS inhibitor 1400W further improves contractile function in reperfused skeletal muscle: J.U. Barker, et al.; Microsurgery 25, 338 (2005), Abstract;
Increased vasoconstriction to noradrenaline by 1400W, inhibitor of iNOS, in rats with streptozotocin-induced diabetes: X. Cheng & C.C. Pang; Eur. J. Pharmacol. 484, 263 (2004), Abstract;
Structural basis for the specificity of the nitric-oxide synthase inhibitors W1400 and Nomega-propyl-L-Arg for the inducible and neuronal isoforms: R. Fedorov, et al.; J. Biol. Chem. 278, 45818 (2003), Abstract; Full Text
Nitric Oxide Ameliorates Hydrophobic Bile Acid-induced Apoptosis in Isolated Rat Hepatocytes by Non-mitochondrial Pathways: E. Gumpricht, et al.; J. Biol. Chem. 277, 25823 (2002), Abstract; Full Text
Nitric oxide synthases: structure, function and inhibition: W.K. Alderton, et al.; Biochem. J. 357, 593 (2001), Review, Abstract; Full Text
The inhibitory potency and selectivity of arginine substrate site nitric-oxide synthase inhibitors is solely determined by their affinity toward the different isoenzymes: R. Boer, et al.; Mol. Pharmacol. 58, 1026 (2000), Abstract; Full Text
1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo: E.P. Garvey, et al.; J. Biol. Chem. 272, 4959 (1997), Abstract; Full Text
Actions of isoform-selective and non-selective nitric oxide synthase inhibitors on endotoxin-induced vascular leakage in rat colon: F. Laszlo & B.J.R. Whittle; Eur. J. Pharmacol. 334, 99 (1997), Abstract;
Selective inhibition of inducible nitric oxide synthase inhibits tumor growth in vivo: studies with 1400W, a novel inhibitor: L.L. Thomsen, et al.; Cancer Res. 57, 3300 (1997), Abstract;

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