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NOS Inhibitors (NOS Induction & Enzyme Activity)
You are here: Product Lines > Nitric Oxide Pathway > Nitric Oxide Synthases [NOS] / Related Products > NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-270-269 Revised 25-May-07
GW 274150 - Discontinued Due to Patent Restrictions
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SYNONYMS (S)-2-Amino-(1-iminoethylamino)-5-thioheptanoic acid
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-270-269-M001   1 mg Inquire
Product Specification
FORMULA: C8H17N3O2S . 2CF3COOH
MW: 219.3 . 228.1
PURITY: ≥95%
APPEARANCE: Yellowish oil.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of inducible nitric oxide synthase (iNOS/NOS II) that is potent (Ki=100nM for human iNOS (NOS II)), long-acting and highly selective (over eNOS (NOS III) >250-fold, over nNOS (NOS I) >80-fold).
Product Specific Literature References
GW274150 is a potent, long-acting, highly selective inhibitor of iNOS (NOS-2) with therapeutical potential in post-operative ileus: W. Alderton, et al.; Acta Physiol. Scand. 167 Suppl., O-36 (1999)
Inhibition of inducible nitric oxide synthase by acetamidine derivatives of hetero-substituted lysine and homolysine: R.J. Young, et al.; Bioorg. Med. Chem. Lett. 10, 597 (2000) Abstract
Nitric oxide synthases: structure, function and inhibition: W.K. Alderton, et al.; Biochem. J. 357, 593 (2001), Review Abstract
Beneficial effects of GW274150, a novel, potent and selective inhibitor of iNOS activity, in a rodent model of collagen-induced arthritis: S. Cuzzocrea, et al.; Eur. J. Pharmacol. 453, 119 (2002) Abstract
A novel, potent and selective inhibitor of the activity of inducible nitric oxide synthase (GW274150) reduces the organ injury in hemorrhagic shock: M.C. McDonald, et al.; J. Physiol. Pharmacol. 53, 555 (2002) Abstract; Full Text
GW274150, a potent and highly selective inhibitor of iNOS, reduces experimental renal ischemia/reperfusion injury: P.K. Chatterjee, et al.; Kidney Int. 63, 853 (2003) Abstract
GW274150 inhibits nitric oxide production by primary cultures of rat proximal tubular cells: P.K. Chatterjee, et al.; Med. Sci. Monit. 9, BR357 (2003) Abstract; Full Text
Effects of GW274150, a novel and selective inhibitor of iNOS activity, in acute lung inflammation: L. Dugo, et al.; Br. J. Pharmacol. 141, 979 (2004) Abstract; Full Text
Beneficial effects of GW274150 treatment on the development of experimental colitis induced by dinitrobenzene sulfonic acid: R. Di Paola, et al.; Eur. J. Pharmacol. 507, 281 (2005) Abstract
GW274150 and GW273629 are potent and highly selective inhibitors of inducible nitric oxide synthase in vitro and in vivo: W.K. Alderton, et al.; Br. J. Pharmacol. 145, 301 (2005) Abstract
GW274150, a novel and highly selective inhibitor of the inducible isoform of nitric oxide synthase (iNOS), shows analgesic effects in rat models of inflammatory and neuropathic pain: J. De Alba, et al.; Pain 120, 170 (2006) Abstract
 
 
ALX-350-333 Revised 05-Apr-08
Harpagoside
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-350-333-M005   5 mg 90.00 USD Add To Cart
ALX-350-333-M025   25 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C24H30O11
MW: 494.5
CAS NUMBER: 19210-12-9
SOURCE/HOST: Isolated from Scrophularia ningpoensis Hemsl (Figwort).
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Anti-inflammatory and anti-diabetic compound. Suppresses LPS-induced inducible nitric oxide synthase (iNOS; NOS II) and cyclooxygenase-2 (COX-2) expression through inhibition of NF-κB activation.
Product Specific Literature References
Antiinflammatory effects of different extracts and harpagoside isolated from Scrophularia frutescens: L. D. Garcia, et al.; Farmaco. 51, 443 (1996) Abstract
Physicochemical properties of harpagoside and its in vitro release from Harpagophytum procumbens extract tablets: S. Chrubasik, et al.; Phytomedicine 6, 469 (2000) Abstract
Scropolioside-D2 and harpagoside-B: two new iridoid glycosides from Scrophularia deserti and their antidiabetic and antiinflammatory activity: B. Ahmed, et al.; Biol. Pharm. Bull. 26, 462 (2003) Abstract; Full Text
Downregulation of iNOS expression in rat mesangial cells by special extracts of Harpagophytum procumbens derives from harpagoside-dependent and independent effects: M. Kaszkin, et al.; Phytomedicine 11, 585 (2004) Abstract
High anti-inflammatory activity of harpagoside-enriched extracts obtained from solvent-modified super- and subcritical carbon dioxide extractions of the roots of Harpagophytum procumbens: M. Gunther, et al.; Phytochem. Anal. 17, 1 (2006) Abstract
Harpagoside suppresses lipopolysaccharide-induced iNOS and COX-2 expression through inhibition of NF-kappa B activation: T.H. Huang, et al.; J. Ethnopharmacol. 104, 149 (2006) Abstract
Simultaneous determination of harpagoside and cinnamic acid in rat plasma by high-performance liquid chromatography: application to a pharmacokinetic study: P. Li, et al.; Anal. Bioanal. Chem. 389, 2259 (2007) Abstract
 
 
ALX-350-350 Revised 21-Aug-08
Honokiol
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SYNONYMS 5,3’-Diallyl-2,4’-biphenyldiol
5,3’-Diallyl-2,4’-dihydroxydiphenyl
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Angiogenesis Research
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ALX-350-350-M005   5 mg 40.00 USD Add To Cart
ALX-350-350-M025   25 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C18H18O2
MW: 266.3
CAS NUMBER: 35354-74-6
MERCK INDEX: 14: 4742
SOURCE/HOST: Isolated from Magnolia officinalis.
PURITY: ≥98% (HPLC)
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Potent and highly tolerable antitumor and antiangiogenic compound. Anxiolytic, anti-thrombotic and antibacterial. Shows central depressant effects in vivo. Inhibitor of nitric oxide (NO) and TNF-α production in LPS-activated macrophages by the suppression of inducible nitric oxide synthase (iNOS; NOS II) expression (IC50=6.4µM). Isomeric with magnolol (Prod. No. ALX-350-352). Inhibits NF-κB activation. Potent scavenger of superoxide and peroxyl radicals.
Product Specific Literature References
Pharmacological properties of Magnolol and Honokiol extracted from Magnolia officinalis: Central depressant effects: K. Watanabe, et al.; Planta Med. 49, 103 (1983) Abstract
Identification of magnolol and honokiol as anxiolytic agents in extracts of saiboku-to, an oriental herbal medicine: Y. Maruyama, et al.; J. Nat. Prod. 61, 135 (1998) Abstract
Inhibitors of nitric oxide synthesis and TNF-alpha expression from Magnolia obovata in activated macrophages: H.J. Son, et al.; Planta Med. 66, 469 (2000) Abstract
Down-modulation of Bcl-XL, release of cytochrome c and sequential activation of caspases during honokiol-induced apoptosis in human squamous lung cancer CH27 cells: S.E. Yang, et al.; Biochem. Pharmacol. 63, 1641 (2002) Abstract
Honokiol, a small molecular weight natural product, inhibits angiogenesis in vitro and tumor growth in vivo: X. Bai, et al.; J. Biol. Chem. 278, 35501 (2003) Abstract; Full Text
Honokiol potentiates apoptosis, suppresses osteoclastogenesis, and inhibits invasion through modulation of nuclear factor-kappaB activation pathway: K.S. Ahn, et al.; Mol. Cancer Res. 4, 621 (2006) Abstract; Full Text
Magnolol and honokiol: inhibitors against mouse passive cutaneous anaphylaxis reaction and scratching behaviors: S.J. Han, et al.; Biol. Pharm. Bull. 30, 2201 (2007) Abstract; Full Text
Anti-inflammatory effect of honokiol is mediated by PI3K/Akt pathway suppression: B.H. Kim & J.Y. Cho; Acta Pharmacol. Sin. 29, 113 (2008) Abstract
Honokiol is a potent scavenger of superoxide and peroxyl radicals: S. Dikalov, et al.; Biochem. Pharmacol. 76, 589 (2008) Abstract
Related Products
 
 
ALX-106-004 Revised 11-Jun-08
NG-Hydroxy-L-arginine . monoacetate
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SYNONYMS L-HOArg . AcOH
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-106-004-M005   5 mg 70.00 USD Add To Cart
ALX-106-004-M025   25 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C6H14N4O3 . CH3COOH
MW: 190.2 . 60.1
CAS NUMBER: 53598-01-9
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Intermediate in the biosynthesis of nitric oxide from L-arginine by nitric oxide synthases (NOS). Inhibitor of arginases.
Product Specific Literature References
Macrophage oxidation of L-arginine to nitrite and nitrate: nitric oxide is an intermediate: M.A. Marletta, et al.; Biochemistry 27, 8706 (1988) Abstract
P.L. Feldman; THL 32, 875 (1991), [Synthesis]
On the substrate specificity of nitric oxide synthase: M. Hecker, et al.; FEBS Lett. 294, 221 (1991) Abstract
N omega-hydroxy-L-arginine is an intermediate in the biosynthesis of nitric oxide from L-arginine: D.J. Stuehr, et al.; J. Biol. Chem. 266, 6259 (1991) Abstract; Full Text
Synthesis and bioactivity of N omega-hydroxyarginine: a possible intermediate in the biosynthesis of nitric oxide from arginine: G.C. Wallace & J.M. Fukuto; J. Med. Chem. 34, 1746 (1991), [Synthesis] Abstract
Nitric oxide and another potent vasodilator are formed from NG-hydroxy- L-arginine by cultured endothelial cells: A. Zembowicz, et al.; PNAS 88, 11172 (1991) Abstract
N omega-hydroxy-L-arginine: a novel arginine analog capable of causing vasorelaxation in bovine intrapulmonary artery: G.C. Wallace, et al.; BBRC 176, 528 (1991) Abstract
Mechanistic probes of N-hydroxylation of L-arginine by the inducible nitric oxide synthase from murine macrophages: R.A. Pufahl, et al.; Biochemistry 31, 6822 (1992), [Synthesis] Abstract
Inhibition of rat liver arginase by an intermediate in NO biosynthesis, NG-hydroxy-L-arginine: implications for the regulation of nitric oxide biosynthesis by arginase: F. Daghigh, et al.; BBRC 202, 174 (1994) Abstract
N omega-hydroxyl-L-arginine, an intermediate in the L-arginine to nitric oxide pathway, is a strong inhibitor of liver and macrophage arginase: J.-L. Boucher, et al.; BBRC 203, 1614 (1994) Abstract
Exogenous NG-hydroxyl-L-arginine causes nitrite production in vascular smooth muscle cells in the absence of nitric oxide synthase activity: C.A. Schott, et al.; FEBS Lett. 341, 203 (1994) Abstract
Inhibition of purified nitric oxide synthase from rat cerebellum and macrophage by L-arginine analogs: Y. Komori, et al.; Arch. Biochem. Biophys. 315, 213 (1994) Abstract
Inhibition of arginase by NG-hydroxy-L-arginine in alveolar macrophages: implications for the utilization of L-arginine for nitric oxide synthesis: M. Hecker, et al.; FEBS Lett. 359, 251 (1995) Abstract
Arginase activity in endothelial cells: inhibition by NG-hydroxy-L-arginine during high-output NO production: G.M. Buga, et al.; Am. J. Physiol. 271, H1988 (1996) Abstract
NG-hydroxy-L-arginine and nitric oxide inhibit Caco-2 tumor cell proliferation by distinct mechanisms: G.M. Buga, et al.; Am. J. Physiol. 275, R1256 (1998) Abstract; Full Text
Further Categories Containing This Product:
Arginine & Arginases / Related Products
 
 
ALX-420-001 Revised 13-Sep-06
Hydroxyguanidine . hemisulfate
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PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-420-001-M025   25 mg 80.00 USD Add To Cart
Product Specification
FORMULA: CH5N3O . 0.5 H2SO4
MW: 75.1 . 49.0
APPEARANCE: White solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Structural analog of NG-hydroxy-L-arginine that potentiates and stabilizes the relaxant effect of nitric oxide.
Product Specific Literature References
Potentiation of the vasorelaxant activity of nitric oxide by hydroxyguanidine: implications for the nature of endothelium-derived relaxing factor: A. Zembowicz, et al.; Br. J. Pharmacol. 107, 1001 (1992) Abstract
Chemical oxidation of N-hydroxyguanidine compounds. Release of nitric oxide, nitroxyl and possible relationship to the mechanism of biological nitric oxide generation: J.M. Fukuto, et al.; Biochem. Pharmacol. 43, 607 (1992) Abstract
Oxidation of N-hydroxyguanidine by nitric oxide and the possible generation of vasoactive species: J. Yoo & J.M. Fukuto; Biochem. Pharmacol. 50, 1995 (1995) Abstract
Nitric oxide involvement in the toxicity of hydroxyguanidine in leukaemia HL60 cells: S.A. Everett, et al.; Br. J. Cancer Suppl. 27, S172 (1996) Abstract
Oxidative denitrification of the antitumour drug hydroxyguanidine: S.A. Everett, et al.; Free Radic. Biol. Med. 24, 1 (1998) Abstract
Identification of an N-hydroxyguanidine reducing activity of xanthine oxidase: M. Dambrova, et al.; Eur. J. Biochem. 257, 178 (1998) Abstract
Hydroxyguanidines inhibit peroxynitrite-induced oxidation: G.J. Southan, et al.; Free Radic. Biol. Med. 25, 914 (1998) Abstract
Unusual oxidative chemistry of N(omega)-hydroxyarginine and N-hydroxyguanidine catalyzed at an engineered cavity in a heme peroxidase: J. Hirst & D.B. Goodin; J. Biol. Chem. 275, 8582 (2000) Abstract; Full Text
Oxidations of N(omega)-hydroxyarginine analogues and various N-hydroxyguanidines by NO synthase II: key role of tetrahydrobiopterin in the reaction mechanism and substrate selectivity: C. Moali, et al.; Chem. Res. Toxicol. 14, 202 (2001) Abstract
 
 
ALX-430-008 Revised 03-Mar-05
2-Iminobiotin
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SYNONYMS Guanidinobiotin
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-430-008-M010   10 mg 25.00 USD Add To Cart
ALX-430-008-M050   50 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C10H17N3O2S
MW: 243.3
CAS NUMBER: 13395-35-2
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 0.1N hydrochloric acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Reversible inhibitor of mouse inducible and rat neuronal nitric oxide synthase (iNOS/NOS II; nNOS/NOS I).
Product Specific Literature References
2-Iminobiotin is an inhibitor of nitric oxide synthases: S.J. Sup, et al.; BBRC 204, 962 (1994) Abstract
Further Categories Containing This Product:
Biotin-(Strept)avidin Systems Other Products
 
 
ALX-270-211 Revised 07-Jun-06
2-Imino-4-methylpiperidine . acetate
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PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-270-211-M005   5 mg 30.00 USD Add To Cart
ALX-270-211-M025   25 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C6H12N2 . CH3COOH
MW: 112.2 . 60.2
CAS NUMBER: 165383-72-2
PURITY: ≥98%
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in PBS, 100% ethanol, methanol, DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Specific inhibitor of inducible nitric oxide synthase (iNOS; NOS II).
 
 
ALX-380-124 Revised 20-Jun-08
Iromycin A
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SYNONYMS 6-(3,7-Dimethyl-octa-2,5-dienyl)-4-hydroxy-3-methyl-5-propyl-1H-pyridin-2-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Nitric Oxide Pathway Modulators
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ALX-380-124-MC05   0.5 mg 180.00 USD Add To Cart
ALX-380-124-M001   1 mg 260.00 USD Add To Cart
ALX-380-124-M005   5 mg 780.00 USD Add To Cart
Product Specification
FORMULA: C19H29NO2
MW: 303.5
SOURCE/HOST: Isolated from Streptomyces bottropensis.
PURITY: ≥98%
APPEARANCE: Off-white to greenish solid.
SOLUBILITY: Soluble in DMSO; fairly soluble in methanol; poorly soluble in acetone.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Pyridone metabolite. Inhibitor of nitric oxide synthases (NOS) showing selectivity for eNOS (NOS III) versus nNOS (NOS I). Inhibitor of thaxtomine biosynthesis and of mitochondrial electron transport chain.
Product Specific Literature References
The iromycins, a new family of pyridone metabolites from Streptomyces sp. I. Structure, NOS inhibitory activity, and biosynthesis: F. Surup, et al; J. Org. Chem. 72, 5085 (2007) Abstract
Iromycins: a new family of pyridone metabolites from Streptomyces sp. II. Convergent total synthesis: H. Shojaei, et al.; J. Org. Chem. 72, 5091 (2007) Abstract
Iromycins from Streptomyces sp. and from synthesis: New inhibitors of the mitochondrial electron transport chain: F. Surup, et al.; Bioorg. Med. Chem. 16, 1738 (2008) Abstract
Further Categories Containing This Product:
NOS Inhibitors (NOS Induction & Enzyme Activity)
 
 
ALX-106-016 Revised 06-Jun-06
D-allo-Isoleucine
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PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-106-016-G001   1 g 80.00 USD Add To Cart
Product Specification
FORMULA: C6H13NO2
MW: 131.2
CAS NUMBER: 1509-35-9
RTECS: BA2930000
PURITY: ≥98%
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
Further Categories Containing This Product:
Special Amino Acids
 
 
ALX-106-015 Revised 07-Dec-04
L-allo-Isoleucine
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PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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Product Numbers: Format: