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PPAR Agonists
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ALX-350-361 Revised 17-Mar-08
Auraptene
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SYNONYMS 7-Geranyloxycoumarin
7-[(2E)-3,7-Dimethylocta-2,6-dienoxy]chromen-2-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Chemopreventive Agents
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ALX-350-361-M005   5 mg 25.00 USD Add To Cart
ALX-350-361-M025   25 mg 75.00 USD Add To Cart
Product Specification
FORMULA: C19H22O3
MW: 298.4
CAS NUMBER: 495-02-3
SOURCE/HOST: Isolated from citrus fruit.
PURITY: ≥98% (HPLC)
SOLUBILITY: Soluble in methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
IDENTITY: Identity determined by NMR.

Product Description
Anti-inflammatory and chemopreventive compound. Exerts tumor preventive effects through apoptosis. Suppresses cell proliferation and lipid peroxidation. Acts as an agonist of PPARs. Induces phase II drug-metabolizing enzymes.
Product Specific Literature References
Citrus auraptene exerts dose-dependent chemopreventive activity in rat large bowel tumorigenesis: the inhibition correlates with suppression of cell proliferation and lipid peroxidation and with induction of phase II drug-metabolizing enzymes: T. Tanaka, et al.; Cancer Res. 58, 2550 (1998) Abstract; Full Text
Immunomodulatory action of citrus auraptene on macrophage functions and cytokine production of lymphocytes in female BALB/c mice: T. Tanaka, et al.; Carcinogenesis 20, 1471 (1999) Abstract; Full Text
Cell proliferation in cancer prevention; effects of preventive agents on estrogen-related endometrial carcinogenesis model and on an in vitro model in human colorectal cells: H. Mori, et al.; Mutat. Res. 480-481, 201 (2001) Abstract
Synthesis and anti-inflammatory activity of natural and semisynthetic geranyloxycoumarins: M. Curini, et al.; Bioorg. Med. Chem. Lett. 14, 2241 (2004) Abstract
Citrus auraptene targets translation of MMP-7 (matrilysin) via ERK1/2-dependent and mTOR-independent mechanism: K. Kawabata, et al.; FEBS Lett. 580, 5288 (2006) Abstract
Citrus auraptene acts as an agonist for PPARs and enhances adiponectin production and MCP-1 reduction in 3T3-L1 adipocytes: K. Kuroyanagi, et al.; BBRC 366, 219 (2008) Abstract
Further Categories Containing This Product:
PPAR Agonists • Natural Products - Anti-inflammatory Agents • Natural Products - Apoptosis Inducers & Inhibitors • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-301-013 Revised 08-Jul-08
Azelaoyl-PAF
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SYNONYMS 1-O-Hexadecyl-2-O-(9-carboxyoctanoyl)-sn-glyceryl-3-phosphocholine
PRODUCT LINE Inflammation
PRODUCT CATEGORY Platelet Activating Factors [PAF] & Receptors / Related Products
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ALX-301-013-M001   1 mg 58.00 USD Add To Cart
ALX-301-013-M005   5 mg 261.00 USD Add To Cart
Product Specification
FORMULA: C33H66NO9P
MW: 651.9
SOURCE/HOST: Synthetic.
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: Soluble in DMSO (8mg/ml) or dimethyl formamide (33mg/ml) or PBS, pH 7.2 (10mg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description
Potent PPARγ agonist which competes for the thiazoladinedione binding site. More potent than 15-deoxy-Δ12,14-prostaglandin J2 (Prod. No. ALX-340-022) and equipotent with rosiglitazone (Prod. No. ALX-350-125) as a ligand for this receptor.
Product Specific Literature References
Oxidized alkyl phospholipids are specific, high affinity peroxisome proliferator-activated receptor gamma ligands and agonists: S.S. Davies, et al.; J. Biol. Chem. 276, 16015 (2001) Abstract; Full Text
General Information
BACKGROUND/TECHNICAL INFORMATION To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Phospholipids / Related Products • PPAR Agonists
 
 
ALX-270-264 Revised 17-Apr-08
Carnosic acid
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-270-264-M010   10 mg 45.00 USD Add To Cart
ALX-270-264-M050   50 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C20H28O4
MW: 332.4
CAS NUMBER: 3650-09-7
SOURCE/HOST: Isolated from Rosmarinus officinalis.
PURITY: ≥95%
APPEARANCE: Yellow powder.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Naturally occurring phenolic compound with antioxidant properties. Inhibits lipid peroxidation induced by NADH or NADPH oxidation. Peroxisome proliferator-activated receptor γ (PPARγ) activator. Anti-inflammatory. Antimicrobial.
Product Specific Literature References
Antioxidative constituents of Rosmarinus officinalis and Salvia officinalis. II. Isolation of carnosic acid and formation of other phenolic diterpenes: K. Schwarz & W. Ternes; Z. Lebensm. Unters. Forsch. 195, 99 (1992) Abstract
Antioxidant and pro-oxidant properties of active rosemary constituents: carnosol and carnosic acid: O.I. Aruoma, et al.; Xenobiotica 22, 257 (1992) Abstract
Radical intermediates and antioxidants: an ESR study of radicals formed on carnosic acid in the presence of oxidized lipids: M. Geoffroy, et al.; Free Radic. Res. 21, 247 (1994) Abstract
Inhibition of lipid peroxidation and superoxide generation by diterpenoids from Rosmarinus officinalis: H. Haraguchi, et al.; Planta Med. 61, 333 (1995) Abstract
Rosemary components inhibit benzo[a]pyrene-induced genotoxicity in human bronchial cells: E.A. Offord, et al.; Carcinogenesis 16, 2057 (1995) Abstract
Chemiluminescence determination of the in vivo and in vitro antioxidant activity of RoseOx and carnosic acid: A.I. Kuzmenko, et al.; J. Photochem. Photobiol. B 48, 63 (1999) Abstract
Carnosic acid and carnosol, phenolic diterpene compounds of the labiate herbs rosemary and sage, are activators of the human peroxisome proliferator-activated receptor gamma: O. Rau, et al.; Planta Med. 72, 881 (2006) Abstract
Potentiation of antimicrobial activity of aminoglycosides by carnosol from Salvia officinalis: K. Horiuchi, et al.; Biol. Pharm. Bull. 30, 287 (2007) Abstract
Further Categories Containing This Product:
Lipid Peroxidation • Active Substances from Fruit and Vegetables • Natural Products with Antibiotic Activity • Natural Products - Anti-inflammatory Agents • PPAR Agonists
 
 
ALX-270-255 Revised 14-Sep-07
Ciglitazone
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SYNONYMS (±)-5-[4-(1-Methylcyclohexylmethoxy)benzyl]-thiazolidine-2,4-dione
U-63287
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-270-255-M001   1 mg 30.00 USD Add To Cart
ALX-270-255-M005   5 mg 80.00 USD Add To Cart
ALX-270-255-M025   25 mg 310.00 USD Add To Cart
Product Specification
FORMULA: C18H23NO3S
MW: 333.5
CAS NUMBER: 74772-77-3
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.

Product Description
Selective PPARγ agonist.
Product Specific Literature References
The structure-activity relationship between peroxisome proliferator-activated receptor gamma agonism and the antihyperglycemic activity of thiazolidinediones: T.M. Willson, et al.; J. Med. Chem. 39, 665 (1996) Abstract; Full Text
Detection and functional characterisation of the transcription factor peroxisome proliferator-activated receptor gamma in lutein cells: B. Löhrke, et al.; J. Endocrinol. 159, 429 (1998) Abstract; Full Text
Peroxisome proliferator-activated receptor gamma ligands are potent inhibitors of angiogenesis in vitro and in vivo: X. Xin, et al.; J. Biol. Chem. 274, 9116 (1999) Abstract; Full Text
Thiazolidinediones--the new insulin enhancers: R.J. Jha; Clin. Exp. Hypertens. 21, 157 (1999), (Review) Abstract
The nuclear receptor PPAR gamma and immunoregulation: PPAR gamma mediates inhibition of helper T cell responses: R.B. Clark, et al.; J. Immunol. 164, 1364 (2000) Abstract; Full Text
Further Categories Containing This Product:
Antidiabetic Agents / Related Products
 
 
ALX-270-475 Revised 17-Jan-08
Ciprofibrate
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SYNONYMS 2-[4-(2,2-Dichlorocyclopropyl)phenoxy]-2-methylpropanoic acid
PRODUCT LINE Obesity & Adipokines
PRODUCT CATEGORY Cholesterol & Lipid Transport / Related Products
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ALX-270-475-M025   25 mg 50.00 USD Add To Cart
ALX-270-475-M100   100 mg 150.00 USD Add To Cart
ALX-270-475-M250   250 mg 300.00 USD Add To Cart
Product Specification
FORMULA: C13H14Cl2O3
MW: 289.2
CAS NUMBER: 52214-84-3
MERCK INDEX: 14: 2313
RTECS: UF0880000
PURITY: ≥98% (HPLC)
APPEARANCE: White to light yellow powder.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: TOXIC. MAY BE CARCINOGENIC.

Product Description
Hypolipidemic compound. PPARα (peroxisome proliferator-activated receptor α) agonist.
Product Specific Literature References
Comparison of the effects of various peroxisome proliferators on peroxisomal enzyme activities, DNA synthesis, and apoptosis in rat and human hepatocyte cultures: V. Goll, et al.; Toxicol. Appl. Pharmacol. 160, 21 (1999) Abstract
Phosphorylation of peroxisome proliferator-activated receptor alpha in rat Fao cells and stimulation by ciprofibrate: P. Passilly, et al.; Biochem. Pharmacol. 58, 1001 (1999) Abstract
Differences in cell proliferation in rodent and human hepatic derived cell lines exposed to ciprofibrate: M.C. Clemencet, et al.; Cancer Lett. 222, 217 (2005) Abstract
P450 CYP2C epoxygenase and CYP4A ω-hydroxylase mediate ciprofibrate-induced PPARα-dependent peroxisomal proliferation: A. Gatica, et al.; J. Lipid Res. 48, 924 (2007) Abstract; Full Text
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Further Categories Containing This Product:
PPAR Agonists • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-270-256 Revised 28-Apr-05
Clofibrate
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SYNONYMS 2-(p-Chlorophenoxy)-2-methylpropionic acid ethyl ester
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-270-256-M500   500 mg 15.00 USD Add To Cart
ALX-270-256-G001   1 g 25.00 USD Add To Cart
Product Specification
FORMULA: C12H15ClO3
MW: 242.7
CAS NUMBER: 637-07-0
MERCK INDEX: 14: 2377
PURITY: ≥98%
APPEARANCE: Colorless oil.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Solutions are stable for up to 6 months when stored at –20°C.

Product Description
Activates PPARα and induces cytochrome P450 4A1 and 4A3.
Product Specific Literature References
Fatty acids activate a chimera of the clofibric acid-activated receptor and the glucocorticoid receptor: M. Göttlicher, et al.; PNAS 89, 4653 (1992) Abstract
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Further Categories Containing This Product:
Cytochrome P450 [CYP450] / Related Products • Carcinogens & Tumor Promoters Other Products • Apoptosis Inducers & Inhibitors Other Products
 
 
ALX-340-010 Revised 28-Feb-07
ETYA
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SYNONYMS 5,8,11,14-Eicosatetraynoic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Lipoxygenases / Related Products
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ALX-340-010-M005   5 mg 40.00 USD Add To Cart
ALX-340-010-M025   25 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C20H24O2
MW: 296.5
CAS NUMBER: 1191-85-1
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, methanol, DMSO, acetone or acetonitrile.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: We do not recommend storing the solutions for more than one day.
HANDLING: Protect from light and oxygen.
HAZARD: TOXIC.

Product Description
Inhibits arachidonic acid uptake. Inhibitor of lipoxygenases, cyclooxygenases (COX), phospholipase A2 and cytochrome P450. Modulates Ca2+ entry into cells. Stimulates luteinizing hormone release from cultured pituitary cells. PPAR agonist.
Product Specific Literature References
Structural requirements of acetylenic fatty acids for inhibition of soybean lipoxygenase and prostaglandin synthetase: D.T. Downing, et al.; Biochim. Biophys. Acta 280, 343 (1972) Abstract
The effect of 5,8,11,14-eicosatetraynoic acid on lipid metabolism: L.D. Tobias & J.G. Hamilton; Lipids 14, 181 (1979) Abstract
An inhibitor of arachidonic acid metabolism stimulates luteinizing hormone (LH) release from cultured pituitary cells: P.M. Conn, et al.; Prostaglandins 19, 873 (1980) Abstract
Evidence for inhibition of leukotriene A4 synthesis by 5,8,11,14-eicosatetraynoic acid in guinea pig polymorphonuclear leukocytes: G.M. Bokoch & P.W. Reed; J. Biol. Chem. 256, 4156 (1981) Abstract; Full Text
Phospholipase A2-induced rat mast cell secretion. Role of arachidonic acid metabolites: E.Y. Chi, et al.; Lab. Invest. 47, 579 (1982) Abstract
Epoxyeicosatrienoic acids stimulate glucagon and insulin release from isolated rat pancreatic islets: J.R. Falck, et al.; BBRC 114, 743 (1983) Abstract
The mechanism of inactivation of lipoxygenases by acetylenic fatty acids: H. Kühn, et al.; Eur. J. Biochem. 139, 577 (1984) Abstract
Comparative effects of indomethacin, acetylenic acids, 15-HETE, nordihydroguaiaretic acid and BW755C on the metabolism of arachidonic acid in human leukocytes and platelets: H. Salari, et al.; Prostagl. Leukotr. Med. 13, 53 (1984) Abstract
Incorporation of 5,8,11,14-eicosatetraynoic acid (ETYA) into cell lipids: competition with arachidonic acid for esterification: A.S. Taylor, et al.; Prostaglandins 29, 449 (1985) Abstract
Inhibition of U937 eicosanoid and DNA synthesis by 5,8,11,14- eicosatetraynoic acid, an inhibitor of arachidonic acid metabolism and its partial reversal by leukotriene C4: F. Ondrey, et al.; Cancer Res. 49, 1138 (1989) Abstract
Effects of 5,8,11,14-eicosatetraynoic acid on thapsigargin-induced calcium entry, and intracellular pH in thyroid FRTL-5 cells: E. Ekokoski & K. Tornquist; Biochim. Biophys. Acta 1223, 274 (1994) Abstract
Further Categories Containing This Product:
Cytochrome P450 [CYP450] / Related Products • PPAR Agonists • PLA2 Inhibitors • Ca2+ Modulators • COX Inhibitors
 
 
ALX-270-481 Revised 11-Aug-08
Fenofibrate
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SYNONYMS 2-[4-(4-Chlorobenzoyl)phenoxy]-2-methyl-propanoic acid 1-methylethyl ester
Procetofen
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-270-481-G005   5 g 30.00 USD Add To Cart
Product Specification
FORMULA: C20H21ClO4
MW: 360.8
CAS NUMBER: 49562-28-9
MERCK INDEX: 14: 3978
RTECS: UA2453400
PURITY: ≥98% (UPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in acetone, ether, DMSO or dimethyl formamide; slightly soluble in 100% ethanol or methanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Hypolipidemic compound. PPARα (peroxisome proliferator-activated receptor α) agonist (EC50=18µM for mouse and EC50=30µM for human PPARα). Also binds to PPARγ, but with at least 10-fold less affinity and is inactive at PPARδ (up to EC50=100µM).
Product Specific Literature References
Inhibition of membrane-bound hepatic 3 hydroxy-3 methyl glutaryl CoA reductase as the consequence of altered membrane fluidity: E. Wulfert, et al.; Artery 9, 120 (1981) Abstract
Fenofibrate protects lipoproteins from lipid peroxidation: synergistic interaction with alpha-tocopherol: E. Chaput, et al.; Lipids 34, 497 (1999) Abstract
Effects of chronic treatment with statins and fenofibrate on rat skeletal muscle: a biochemical, histological and electrophysiological study: S. Pierno, et al.; Br. J. Pharmacol. 149, 909 (2006) Abstract; Full Text
In vitro and in vivo effects of the PPAR-alpha agonists fenofibrate and retinoic acid in endometrial cancer: S.A. Saidi, et al.; Mol. Cancer 5, 13 (2006) Abstract; Full Text
PPARalpha agonist fenofibrate suppresses tumor growth through direct and indirect angiogenesis inhibition: D. Panigrahy, et al.; PNAS 105, 985 (2008) Abstract; Full Text
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ALX-420-029 Revised 22-Feb-08
GW1929
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SYNONYMS N-(2-Benzoylphenyl)-L-tyrosine PPARγ Agonist
(2S)-((2-Benzoylphenyl)amino-3-[4-[2-(methylpyridin-2-ylamino)ethoxy]phenyl)propionic acid
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-420-029-M001   1 mg 80.00 USD Add To Cart
ALX-420-029-M005   5 mg 360.00 USD Add To Cart
Product Specification
FORMULA: C30H29N3O4
MW: 495.6
PURITY: ≥97%
APPEARANCE: Off-white to yellow crystalline solid.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Potent (<10nM) and subtype-selective (>1'000-fold) PPARγ agonist which does not contain a thiazolidinedione moiety. The glucose-lowering effect of GW1929 in rats is 100-fold more potent than that of troglitazone (Prod. No. ALX-270-355).
Product Specific Literature References
N-(2-Benzoylphenyl)-L-tyrosine PPARgamma agonists. 1. Discovery of a novel series of potent antihyperglycemic and antihyperlipidemic agents: B.R. Henke, et al.; J. Med. Chem. 41, 5020 (1998) Abstract
Superoxide anion-dependent Raf/MEK/ERK activation by peroxisome proliferator activated receptor gamma agonists 15-deoxy-delta(12,14)-prostaglandin J(2), ciglitazone, and GW1929: W.C. Huang, et al.; Exp. Cell Res. 277, 192 (2002) Abstract
15-Deoxy-{delta}12,14-prostaglandin j2 inhibits interleukin-1{beta}-induced nuclear factor-{kappa}b in human amnion and myometrial cells: mechanisms and implications: T.M. Lindström & P.R. Bennett; J. Clin. Endocrinol. Metab. 90, 3534 (2005) Abstract; Full Text
 
 
ALX-420-032 Revised 21-Nov-08
GW501516
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PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Agonists
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ALX-420-032-M001   1 mg 83.00 USD Add To Cart
ALX-420-032-M005   5 mg 367.00 USD Add To Cart
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Product Specification
FORMULA: C21H18F3NO3S2
MW: 453.5
CAS NUMBER: 317318-70-0
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (50mg/ml), dimethyl formamide (25mg/ml), 100% ethanol (12mg/ml) or methanol (50mg/ml); slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR, 13C-NMR and MS.

Product Description
Specific agonist for PPARδ (EC50=1.1nM) with a 1'000-fold selectivity over the other human subtypes.
Product Specific Literature References
A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport: W.R. Oliver, Jr., et al.; PNAS 98, 5306 (2001) Abstract;