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COX Inhibitors
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ALX-385-034 Revised 01-Dec-08 New product
Pterostilbene
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SYNONYMS trans-3,5-Dimethoxy-4’-hydroxystilbene
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-385-034-M025   25 mg 90.00 USD Add To Cart
ALX-385-034-M100   100 mg 270.00 USD Add To Cart
ALX-385-034-M500   500 mg 750.00 USD Add To Cart
Product Specification
FORMULA: C16H16O3
MW: 256.3
CAS NUMBER: 537-42-8
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white to light brown powder.
SOLUBILITY: Soluble in DMSO (20mg/ml) or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and oxygen.
HAZARD: IRRITANT.
IDENTITY: Identity determined by MS and 1H-NMR.
MELTINGPOINT: 92.7-94.6°C

Product Description
Cell permeable natural methoxylated analog of resveratrol (Prod. No. ALX-270-125). Antioxidant, antiproliferative, anti-inflammatory, anti-hyperglycemic and anti-diabetic agent. Induces apoptosis. Inhibits activator protein 1 (AP-1) and NF-κB activation. Moderately inhibits COX-1 and COX-2 (IC50=19.8μM and 83.9μM).
Product Specific Literature References
Antihyperglycemic activity of phenolics from Pterocarpus marsupium: M Manickam, et al.; J. Nat. Prod. 60, 609 (1997) Abstract
Cancer chemopreventive and antioxidant activities of pterostilbene, a naturally occurring analogue of resveratrol: A.M. Rimando, et al.; J. Agric. Food Chem. 50, 3453 (2002) Abstract
Synthesis and biological evaluation of resveratrol and analogues as apoptosis-inducing agents: M. Roberti, et al.; J. Med. Chem. 46, 3546 (2003) Abstract
Antioxidant activity of hydroxystilbene derivatives in homogeneous solution: R. Amorati, et al.; J. Org. Chem. 69, 7101 (2004) Abstract
Association between pterostilbene and quercetin inhibits metastatic activity of B16 melanoma: P. Ferrer, et al.; Neoplasia 7, 37 (2005) Abstract; Full Text
Pterostilbene, a new agonist for the peroxisome proliferator-activated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters: A.M. Rimando, et al.; J. Agric. Food Chem. 53, 3403 (2005) Abstract
Selective COX-2 inhibition by a Pterocarpus marsupium extract characterized by pterostilbene, and its activity in healthy human volunteers: S. Hougee, et al.; Planta Med. 71, 387 (2005) Abstract
Effect of pterostilbene on hepatic key enzymes of glucose metabolism in streptozotocin- and nicotinamide-induced diabetic rats: L. Pari & M.A. Satheesh; Life Sci. 79, 641 (2006) Abstract
Effect of natural analogues of trans-resveratrol on cytochromes P4501A2 and 2E1 catalytic activities: R. Mikstacka, et al.; Xenobiotica 36, 269 (2006) Abstract
The antioxidant role of pterostilbene in streptozotocin-nicotinamide-induced type 2 diabetes mellitus in Wistar rats: M. Amarnath Satheesh & L. Pari; J. Pharm. Pharmacol. 58, 1483 (2006) Abstract
Pharmacometrics of stilbenes: seguing towards the clinic: K.A. Roupe, et al.; Curr. Clin. Pharmacol. 1, 81 (2006) Abstract
Nitric oxide mediates natural polyphenol-induced Bcl-2 down-regulation and activation of cell death in metastatic B16 melanoma: P. Ferrer, et al.; J. Biol. Chem. 282, 2880 (2007) Abstract; Full Text
Pterostilbene, an active constituent of blueberries, suppresses aberrant crypt foci formation in the azoxymethane-induced colon carcinogenesis model in rats: N. Suh, et al.; Clin. Cancer Res. 13, 350 (2007) Abstract; Full Text
Pterostilbene induces apoptosis and cell cycle arrest in human gastric carcinoma cells: M.H. Pan, et al.; J. Agric. Food Chem. 55, 7777 (2007) Abstract
Pharmacometrics of pterostilbene: preclinical pharmacokinetics and metabolism, anticancer, antiinflammatory, antioxidant and analgesic activity: C.M. Remsberg, et al.; Phytother. Res. 22, 169 (2008) Abstract
Identification of molecular pathways affected by pterostilbene, a natural dimethylether analog of resveratrol: Z. Pan, et al.; BMC Med. Genomics 1, 7 (2008) Abstract; Full Text
Pterostilbene is equally potent as resveratrol in inhibiting 12-O-tetradecanoylphorbol-13-acetate activated NFkappaB, AP-1, COX-2, and iNOS in mouse epidermis: M. Cichocki, et al.; Mol. Nutr. Food Res. 52, S62 (2008) Abstract
Pterostilbene suppressed lipopolysaccharide-induced up-expression of iNOS and COX-2 in murine macrophages: M.H. Pan, et al.; J. Agric. Food Chem. 56, 7502 (2008) Abstract
In vitro evaluation of the cytotoxic and anti-proliferative properties of resveratrol and several of its analogs: B. Billack, et al.; Cell. Mol. Biol. Lett. 13, 553 (2008) Abstract
Related Products
Further Categories Containing This Product:
Natural Products - Apoptosis Inducers & Inhibitors • Antidiabetic Agents / Related Products • Natural Products - Anti-inflammatory Agents • COX Inhibitors • Natural Products - NF-kB Pathway Inhibitors • Stilbenoids
 
 
ALX-270-125 Revised 25-Apr-08
Resveratrol
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SYNONYMS trans-3,4’,5-Trihydroxystilbene
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-125-M050   50 mg 36.00 USD Add To Cart
ALX-270-125-M100   100 mg 50.00 USD Add To Cart
ALX-270-125-M250   250 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C14H12O3
MW: 228.2
CAS NUMBER: 501-36-0
MERCK INDEX: 14: 8158
SOURCE/HOST: Isolated from Polygonum cuspidatum.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: ~65mg/ml soluble in DMSO, 100% ethanol or dimethyl formamide; slightly soluble in PBS, pH 7.2 (~100 µg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: IRRITANT.

Product Description
Shows cancer chemopreventive activity. Specific inhibitor of cyclooxygenase-1 (COX-1). Inhibits the hydroperoxidase activity of COX-1. Antioxidant. Potent activator of human deacetylase SIRT1. Protects against 4-hydroxynonenal (4-HNE) induced oxidative stress and apoptosis.
Product Specific Literature References
Vasorelaxing activity of resveratrol and quercetin in isolated rat aorta: C.K. Chen, et al.; Gen. Pharmacol. 27, 363 (1996) Abstract
Cancer chemopreventive activity of resveratrol, a natural product derived from grapes: M. Jang, et al.; Science 275, 218 (1997) Abstract
Cancer chemopreventive activity of resveratrol: M. Jang & J.M. Pezzuto; Drugs Exp. Clin. Res. 25, 65 (1999) Abstract
Capillary electrophoresis determination, synthesis, and stability of resveratrol and related 3-O-beta-D-glucopyranosides: V. Brandolini, et al.; J. Agric. Food Chem. 50, 7407 (2002) Abstract
Small molecule activators of sirtuins extend Saccharomyces cerevisiae lifespan: K.T. Howitz, et al.; Nature 425, 191 (2003) Abstract
Resveratrol protects against 4-HNE induced oxidative stress and apoptosis in Swiss 3T3 fibroblasts: O. Kutuk, et al.; Biofactors 20, 1 (2004) Abstract
Resveratrol, a polyphenol found in grapes, suppresses oxidative damage and stimulates apoptosis during early colonic inflammation in rats: A.R. Martin, et al.; Biochem. Pharmacol. 67, 1399 (2004) Abstract
Resveratrol interferes with AKT activity and triggers apoptosis in human uterine cancer cells: E. Sexton, et al.; Mol. Cancer 5, 45 (2006) Abstract
Resveratrol and its analogs: Defense against cancer, coronary disease and neurodegenerative maladies or just a fad?: P. Saiko, et al.; Mutat. Res. 658, 68 (2008) Abstract
Related Products
Further Categories Containing This Product:
Natural Products - Chemopreventive Agents • Active Substances from Fruit and Vegetables • Stilbenoids • Sirtuins / Related Products • COX Inhibitors
 
 
ALX-350-299 Revised 25-May-07
S14-95
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products for Inflammation Research
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ALX-350-299-MC05   0.5 mg 250.00 USD Add To Cart
Product Specification
FORMULA: C28H34O5
MW: 450.6
SOURCE/HOST: Isolated from Penicillium sp.
PURITY: ≥95% (HPLC)
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
SHORT TERM STORAGE: +4°C
LONG TERM STORAGE: -20°C

Product Description
Potent inhibitor of cytokine-induced activation of STAT1α leading to the inhibition of inducible expression of proinflammatory enzymes (COX-2, iNOS (NOS II)) and cytokines (TNF-α).
Product Specific Literature References
S14-95, a novel inhibitor of the JAK/STAT pathway from a Penicillium species: G. Erkel, et al.; J. Antibiot. 56, 337 (2003) Abstract
Sporogen, S14-95, and S-curvularin, three inhibitors of human inducible nitric-oxide synthase expression isolated from fungi: Y. Yao, et al.; Mol. Pharmacol. 63, 383 (2003) Abstract; Full Text
Further Categories Containing This Product:
NOS Inhibitors (NOS Induction & Enzyme Activity) • MAPK Pathway Inhibitors • Natural Products - Protein Kinase Inhibitors • Natural Products - Nitric Oxide Pathway Modulators • COX Inhibitors
 
 
ALX-270-377 Revised 07-Feb-05
SC-236
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SYNONYMS 4-[5-(4-Chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
PRODUCT LINE Inflammation
PRODUCT CATEGORY COX Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-377-M005   5 mg 70.00 USD Add To Cart
ALX-270-377-M025   25 mg 280.00 USD Add To Cart
Product Specification
FORMULA: C16H11ClF3N3O2S
MW: 401.8
PURITY: ≥95%
APPEARANCE: White to off-white crystalline powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 2 years after receipt when stored at -20°C. Stock solutions are stable for 3 months when stored at -20°C.
HANDLING: Protect from light. Packaged under inert gas.

Product Description
Highly selective and potent inhibitor of cyclooxygenase-2 (IC50=10nM for COX-2 versus IC50=17.8µM for COX-1) with antitumor properties. Exhibits longer half-life time and reduced gastric toxicity in fasting rat model. Has antitumor properties and has been shown to induce apoptosis and bFGF and VEGF-driven angiogenesis. Potent antimetastatic activity against both spontaneous metastases arising following primary tumour excision and experimental metastases.
Product Specific Literature References
A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors: J.K. Gierse, et al.; J. Biol. Chem. 271, 15810 (1996) Abstract; Full Text
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib): T.D. Penning, et al.; J. Med. Chem. 40, 1347 (1997) Abstract
Prostaglandin E(2) mediates inhibition of insulin secretion by interleukin-1beta: P.O. Tran, et al.; J. Biol. Chem. 274, 31245 (1999) Abstract; Full Text
COX-2 inhibitors. A new class of antiangiogenic agents: J.L. Masferrer, et al.; Ann. NY Acad. Sci. 889, 84 (1999) Abstract
Inhibition of cyclooxygenase-2 decreases DNA synthesis induced by platelet-derived growth factor in Swiss 3T3 fibroblasts: E. Castano, et al.; J. Pharmacol. Exp. Ther. 293, 509 (2000) Abstract; Full Text
Enhancement of intrinsic tumor cell radiosensitivity induced by a selective cyclooxygenase-2 inhibitor: C. Petersen, et al.; Clin. Cancer Res. 6, 2513 (2000) Abstract; Full Text
Cyclooxygenase-2-derived prostaglandin E2 and lipoxin A4 accelerate resolution of allergic edema in Angiostrongylus costaricensis-infected rats: relationship with concurrent eosinophilia: C. Bandeira-Melo, et al.; J. Immunol. 164, 1029 (2000) Abstract; Full Text
Cyclooxygenase-2 inhibitor SC-236 attenuates mechanical allodynia following nerve root injury in rats: T.A. Deleo, et al.; J. Orthop. Res. 18, 977 (2000) Abstract
Prostaglandins are required for CREB activation and cellular proliferation during liver regeneration: D.A. Rudnick, et al.; PNAS 98, 8885 (2001) Abstract; Full Text
Protective role of cyclooxygenase inhibitors in the adverse action of passive cigarette smoking on the initiation of experimental colitis in rats: X. Guo, et al.; Eur. J. Pharmacol. 411, 193 (2001) Abstract
Neuroprotection by the selective cyclooxygenase-2 inhibitor SC-236 results in improvements in behavioral deficits induced by reversible spinal cord ischemia: P.A. Lapchak, et al.; Stroke 32, 1220 (2001) Abstract; Full Text
Novel target for induction of apoptosis by cyclo-oxygenase-2 inhibitor SC-236 through a protein kinase C-beta(1)-dependent pathway: X.H. Jiang, et al.; Oncogene 21, 6113 (2002) Abstract
Cyclooxygenase-2 inhibitor (SC-236) suppresses activator protein-1 through c-Jun NH2-terminal kinase: B.C. Wong, et al.; Gastroenterology 126, 136 (2004) Abstract
Further Categories Containing This Product:
Antitumor Agents (Apoptosis Inducers) • Antitumor Agents (Enzyme Inhibitors)
 
 
ALX-270-427 Revised 22-Apr-08
SC-560
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SYNONYMS 5-(4-Chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole
PRODUCT LINE Inflammation
PRODUCT CATEGORY COX Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-427-M005   5 mg 60.00 USD Add To Cart
ALX-270-427-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C17H12N2OClF3
MW: 352.7
CAS NUMBER: 188817-13-2
PURITY: ≥98%
FORMULATION: White to off-white crystalline solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide; sparingly soluble in aqueous buffers.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 2 years after receipt when stored at –20°C.

Product Description
Selective COX-1 inhibitor (IC50=9nM). Shows 700-fold more selectivity over COX-2 (IC50=6.3µM). Inhibits COX-1-derived platelet thromboxane B2, gastric PGE2, and dermal PGE2 production. Orally active in rat.
Product Specific Literature References
Selective inhibition of inducible cyclooxygenase 2 in vivo is antiinflammatory and nonulcerogenic: J.L. Masferrer, et al.; PNAS 91, 3228 (1994) Abstract; Full Text
Pharmacological analysis of cyclooxygenase-1 in inflammation: C.J. Smith, et al.; PNAS 95, 13313 (1998) Abstract; Full Text
 
 
ALX-350-229 Revised 24-Jul-08
Sedanolide
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SYNONYMS 3-Butyl-3a,4,5,6-tetrahydro-1(3H)-isobenzofuranone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-229-M100   100 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C12H18O2
MW: 194.1
CAS NUMBER: 6415-59-4
SOURCE/HOST: Isolated from Apium graveolens L.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol or ethyl acetate.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
MELTINGPOINT: 30-31°C

Product Description
Inducer of glutathione S-transferases and inhibitor of chemically induced carcinogenesis. Mosquitocidal, nematicidal and antifungal. Was shown to inhibit cyclooxygenase-1 and -2 (COX-1 and COX-2) as well as topoisomerase I and topoisomerase II.
Product Specific Literature References
Chemoprevention of benzo[a]pyrene-induced forestomach cancer in mice by natural phthalides from celery seed oil: G.-Q. Zheng, et al.; Nutr. Cancer 19, 77 (1993) Abstract
Mosquitocidal, nematicidal, and antifungal compounds from Apium graveolens L. seeds: R.A. Momin & M.G. Nair; J. Agric. Food Chem. 49, 142 (2001) Abstract
Sedanolide, a natural phthalide from celery seed oil: effect on hydrogen peroxide and tert-butyl hydroperoxide-induced toxicity in HepG2 and CaCo-2 human cell lines: J.A. Woods, et al.; In Vitr. Mol. Toxicol. 14, 233 (2001) Abstract
Antioxidant, cyclooxygenase and topoisomerase inhibitory compounds from Apium graveolens Linn. seeds: R.A. Momin & M.G. Nair; Phytomedicine 9, 312 (2002) Abstract
Further Categories Containing This Product:
Antitumor Agents (Enzyme Activators & Inducers) • Natural Products - Antifungal Agents • Glutathione S-Transferase • Natural Products - Topoisomerase Inhibitors • Active Substances from Fruit and Vegetables • COX Inhibitors
 
 
ALX-430-105 Revised 10-Dec-04
Sulindac
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SYNONYMS MK-231
(1Z)-5-Fluoro-2-methyl-1-[[4-(methylsulfinyl)phenyl]methylene]-1H-indene-3-acetic acid
cis-5-Fluoro-2-methyl-1-[p-(methylsulfinyl)benzylidene]-indene-3-acetic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-430-105-G001   1 g 10.00 USD Add To Cart
Product Specification
FORMULA: C20H17FO3S
MW: 356.4
CAS NUMBER: 38194-50-2
MERCK INDEX: 14: 8982
RTECS: NK8226000
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or aqueous bases.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Inhibits the NF-κB pathway. Non-steroidal anti-inflammatory drug. Reduces the level and activity of several cyclin-dependent kinases (CDKs) and induces apoptosis. For the active metabolite sulindac sulfide see Prod. No. ALX-430-106.
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • Apoptosis Inducers & Inhibitors Other Products • COX Inhibitors
 
 
ALX-430-106 Revised 31-Aug-04
Sulindac sulfide
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PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-106-M005   5 mg 32.00 USD Add To Cart
ALX-430-106-M025   25 mg 85.00 USD Add To Cart
Product Specification
FORMULA: C20H17FO2S
MW: 340.4
CAS NUMBER: 32004-67-4
PURITY: ≥98%
APPEARANCE: Yellow-orange solid.
SOLUBILITY: Soluble in 100% ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Active metabolite of sulindac (Prod. Nr. ALX-430-105). NF-κB inhibitor. Induces apoptosis. Inhibits Ras signaling. Also inhibits cyclooxygenase (COX).
Product Specific Literature References
Antineoplastic drugs sulindac sulfide and sulfone inhibit cell growth by inducing apoptosis: G.A. Piazza, et al.; Cancer Res. 55, 3110 (1995) Abstract
Sulindac sulfide inhibits Ras signaling: C. Herrmann, et al.; Oncogene 17, 1769 (1998) Abstract
Sulindac inhibits activation of the NF-kappaB pathway: Y. Yamamoto, et al.; J. Biol. Chem. 274, 27307 (1999) Abstract; Full Text
Further Categories Containing This Product:
NF-kB Pathway Inhibitors • COX Inhibitors • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-430-107 Revised 20-Aug-08
Sulindac sulfone
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PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-107-M005   5 mg 30.00 USD Add To Cart
ALX-430-107-M050   50 mg