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Nuclear Receptors / Related Products
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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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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-270-356 Revised 04-May-06
GW9662
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SYNONYMS 2-Chloro-5-nitrobenzanilide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY PPAR Antagonists
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-356-M001   1 mg 10.00 USD Add To Cart
ALX-270-356-M005   5 mg 35.00 USD Add To Cart
ALX-270-356-M025   25 mg 140.00 USD Add To Cart
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Product Specification
FORMULA: C13H9N2O3Cl
MW: 276.7
CAS NUMBER: 22978-25-2
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol, DMSO or dimethyl formamide.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Blocks the PPARγ-induced differentiation of monocytes to osteoclasts by >90% at a dose of 0.1µM. Much more potent antagonist than BADGE (Prod. No. ALX-270-353).
Product Specific Literature References
IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor gamma 1: A.C. Bendixen, et al.; PNAS 98, 2443 (2001) Abstract; Full Text
Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662: L.M. Leesnitzer, et al.; Biochemistry 41, 6640 (2002) Abstract
Activation of peroxisome proliferator-activated receptor gamma inhibits osteoprotegerin gene expression in human aortic smooth muscle cells: M. Fu, et al.; BBRC 294, 597 (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%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in acetonitrile, DMSO, dimethyl formamide, 100% ethanol or methanol; slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

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; Full Text
The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells: U. Dressel, et al.; Mol. Endocrinol. 17, 2477 (2003) Abstract
Peroxisome proliferator-activated receptor (PPAR) alpha and PPARbeta/delta, but not PPARgamma, modulate the expression of genes involved in cardiac lipid metabolism: A.J. Gilde, et al.; Circ. Res. 92, 518 (2003) Abstract
PPARdelta activation induces COX-2 gene expression and cell proliferation in human hepatocellular carcinoma cells: B. Glinghammar, et al.; BBRC 308, 361 (2003) Abstract
Novel selective small molecule agonists for peroxisome proliferator-activated receptor delta (PPARdelta)-synthesis and biological activity: M.L. Sznaidman, et al.; Bioorg. Med. Chem. Lett. 13, 1517 (2003) Abstract
Peroxisome-proliferator-activated receptor delta activates fat metabolism to prevent obesity: Y.X. Wang, et al.; Cell 113, 159 (2003) Abstract
A short and efficient synthesis of the pharmacological research tool GW501516 for the peroxisome proliferator-activated receptor delta: Z.L. Wei & A.P. Kozikowski; J. Org. Chem. 68, 9116 (2003) Abstract
 
 
ALX-340-037 Revised 08-Jul-08
8(S)-HETE
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SYNONYMS 8-Hydroxy-[S-(E,Z,Z,Z)]-5,9,11,14-eicosatetraenoic acid
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Hydroxy, Hydroperoxy & Oxo Fatty Acids / Related Products
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ALX-340-037-C025   25 µg 165.00 USD Add To Cart
Product Specification
FORMULA: C20H32O3
MW: 320.5
CAS NUMBER: 98462-03-4
PURITY: ≥98%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in PBS, pH 7.2 (0.8mg/ml) or 0.1M Na2CO3 (2mg/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. Stable for at least 6 months in other organic solvents when stored at -20°C. Keep aqueous solutions on ice and use within 12 hours.
HANDLING: Protect from light and oxygen.

Product Description
Activator of PPARα. Activates mouse skin protein kinase C (PKC).
Product Specific Literature References
Investigation of the mechanism of biosynthesis of 8-hydroxyeicosatetraenoic acid in mouse skin: M.A. Hughes & A.R. Brash; Biochim. Biophys. Acta 1081, 347 (1991) Abstract
In vitro activation of mouse skin protein kinase C by fatty acids and their hydroxylated metabolites: H.H. Lo, et al.; Lipids 29, 547 (1994) Abstract
Differential activation of peroxisome proliferator-activated receptors by eicosanoids: K. Yu, et al.; J. Biol. Chem. 270, 23975 (1995) Abstract; Full Text
Expression of peroxisome proliferator-activated receptors in urinary tract of rabbits and humans: Y. Guan, et al.; Am. J. Physiol. 273, F1013 (1997) Abstract
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:
PPAR Agonists • PKC Activators
 
 
ALX-270-474 Revised 22-Oct-07
HSD Inhibitor 23
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SYNONYMS N-(5-Hydroxytricyclo[3.3.1.13,7]dec-2-yl)-α,α-dimethyl-4-[5-(trifluoromethyl)-2-pyridinyl]-1-piperazineacetamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Glucocorticoids & Glucocorticoid Receptors / Related Products
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ALX-270-474-M001   1 mg 190.00 USD Add To Cart
Product Specification
FORMULA: C24H33F3N4O2
MW: 466.5
CAS NUMBER: 868604-75-5
PURITY: ≥95%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Selective, potent and cell permeable small molecule inhibitor of 11-β-hydroxysteroid dehydrogenase.
Product Specific Literature References
Discovery and metabolic stabilization of potent and selective 2-amino-N-(adamant-2-yl) acetamide 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: J.J. Rohde, et al.; J. Med. Chem. 50, 149 (2007) Abstract; Full Text
 
 
ALX-350-097 Revised 16-Jun-08
Hyperforin . dicyclohexylammonium salt (high purity)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products for Neurological Research
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ALX-350-097-C500   500 µg 130.00 USD Add To Cart
ALX-350-097-M001   1 mg 210.00 USD Add To Cart
Product Specification
FORMULA: C35H51O4 . C12H24N
MW: 535.8 . 182.3
CAS NUMBER: 11079-53-1 (non-salt form)
SOURCE/HOST: Isolated from St. John's wort (Hypericum perforatum).
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white powder.
PURITY DETAIL: Contains <3% adhyperforin.
SOLUBILITY: Soluble in DMSO, methanol or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Keep under inert gas. Protect from light.

Product Description
Major constituent of St. John’s wort, a herbal remedy widely used for the treatment of depression. Inhibits the reuptake of neurotransmitters in synapses. Activator of the pregnane X receptor (PXR), which serves as a key regulator of CYP3A4 transcription, a member of the cytochrome (CYP) P450 enzyme system. Specifically activates TRPC6 channels. Represents an interesting lead-structure for a new class of antidepressants. Displays several other biological properties of potential pharmacological interest, including antibacterial, anti-inflammational, antitumoral and anti-angiogenic effects. Induces apoptosis in various cancer cells.
Product Specific Literature References
Hyperforin as a possible antidepressant component of hypericum extracts: S.S. Chatterjee, et al.; Life Sci. 63, 499 (1998) Abstract
Hyperforin attenuates various ionic conductance mechanisms in the isolated hippocampal neurons of rat: S. Chatterjee, et al.; Life Sci. 65, 2395 (1999) Abstract
Antibacterial activity of hyperforin from St John's wort, against multiresistant Staphylococcus aureus and gram-positive bacteria: C.M. Schempp, et al.; Lancet 353, 2129 (1999) Abstract
Hyperforin, a major antidepressant constituent of St. John's Wort, inhibits serotonin uptake by elevating free intracellular Na+1: A. Singer, et al.; J. Pharmacol. Exp. Ther. 290, 1363 (1999) Abstract
St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor: L.B. Moore, et al.; PNAS 97, 7500 (2000) Abstract
Inhibition of human cytochrome P450 enzymes by constituents of St. John's Wort, an herbal preparation used in the treatment of depression: R.S. Obach; J. Pharmacol. Exp. Ther. 294, 88 (2000) Abstract
St John's wort, a herbal antidepressant, activates the steroid X receptor: J.M. Wentworth, et al.; J. Endocrinol. 166, R11 (2000) Abstract
St John's wort (Hypericum perforatum L.): a review of its chemistry, pharmacology and clinical properties: J. Barnes, et al.; J. Pharm. Pharmacol. 53, 583 (2001), (Review) Abstract
St John's wort: Prozac from the plant kingdom: G. Di Carlo, et al.; TIPS 22, 292 (2001), (Review) Abstract
Effect of St. John's wort on free radical production: E.J. Hunt, et al.; Life Sci. 69, 181 (2001) Abstract
Hypericum perforatum (St John's Wort): a non-selective reuptake inhibitor? A review of the recent advances in its pharmacology: P.J. Nathan; J. Psychopharmacol. 15, 47 (2001), (Review) Abstract
Aristoforin, a novel stable derivative of hyperforin, is a potent anticancer agent: M. Gartner, et al.; Chembiochem 6, 171 (2005) Abstract
Hyperforin, a new lead compound against the progression of cancer and leukemia?: C. Quiney, et al.; Leukemia 20, 1519 (2006), (Review) Abstract
Hyperforin a key constituent of St. John’s wort specifically activates TRPC6 channels: K. Leuner, et al.; FASEB J. 21, 4101 (2007) Abstract
Further Categories Containing This Product:
Other Natural Products - DNA Regulation / Transcription • Pregnane X Receptor [PXR] / Related Products • Natural Products - Anti-inflammatory Agents • Natural Products for Angiogenesis Research • Natural Products - Antitumor Reagents • Natural Products with Antibiotic Activity • Neuroactive Agents Other Products • Antitumor Agents (Apoptosis Inducers) • Natural Products - Apoptosis Inducers & Inhibitors
 
 
ALX-385-025 Revised 07-Apr-08
8-Isopentenylnaringenin
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SYNONYMS 8-Prenylnaringenin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavanones
Ordering Information
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ALX-385-025-M005   5 mg 155.00 USD Add To Cart
Product Specification
FORMULA: C20H20O5
MW: 340.4
SOURCE/HOST: Isolated from hops (Humulus lupulus L.).
PURITY: ≥97% (HPLC)
APPEARANCE: Light yellow powder
SOLUBILITY: Soluble in methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Prenyl flavonoid. Phytoestrogen. Selective, non-steroidal estrogen receptor α (ERα) ligand. Potent inhibitor of angiogenesis in vitro and in vivo. Chemopreventive agent against cancer induced by heterocyclic amines.
Product Specific Literature References
Prenylflavonoids: a new class of non-steroidal phytoestrogen (Part 1). Isolation of 8-isopentenylnaringenin and an initial study on its structure-activity relationship: M. Kitaoka, et al.; Planta Med. 64, 511 (1998) Abstract
Prenylflavonoids: a new class of non-steroidal phytoestrogen (Part 2). Estrogenic effects of 8-isopentenylnaringenin on bone metabolism: M. Miyamoto, et al.; Planta Med. 64, 516 (1998) Abstract
Identification of a potent phytoestrogen in hops (Humulus lupulus L.) and beer: S.R. Milligan, et al.; J. Clin. Endocrinol. Metab. 84, 2249 (1999) Abstract
Prenylflavonoids from hops inhibit the metabolic activation of the carcinogenic heterocyclic amine 2-amino-3-methylimidazo[4, 5-f]quinoline, mediated by cDNA-expressed human CYP1A2: C.L. Miranda, et al.; Drug Metab. Dispos. 28, 1297 (2000) Abstract; Full Text
The endocrine activities of 8-prenylnaringenin and related hop (Humulus lupulus L.) flavonoids: S.R. Milligan, et al.; J. Clin. Endocrinol. Metab. 85, 4912 (2000) Abstract; Full Text
8-prenylnaringenin, a novel phytoestrogen, inhibits angiogenesis in vitro and in vivo: M.S. Pepper, et al.; J. Cell Physiol. 199, 98 (2004) Abstract
Xanthohumol and related prenylflavonoids from hops and beer: to your good health!: J.F. Stevens & J.E. Page; Phytochemistry 65, 1317 (2004), (Review) Abstract
Rapid yeast estrogen bioassays stably expressing human estrogen receptors alpha and beta, and green fluorescent protein: a comparison of different compounds with both receptor types: T.F. Bovee, et al.; J. Steroid Biochem. Mol. Biol. 91, 99 (2004) Abstract
8-Prenylnaringenin, inhibits estrogen receptor-alpha mediated cell growth and induces apoptosis in MCF-7 breast cancer cells: E. Brunelli, et al.; J. Steroid Biochem. Mol. Biol. 107, 140 (2007) Abstract
Further Categories Containing This Product:
Active Substances from Fruit and Vegetables • Estrogen & Estrogen Receptors / Related Products • Natural Products for Angiogenesis Research • Natural Products - Chemopreventive Agents • Other Natural Products - DNA Regulation / Transcription
 
 
ALX-350-279 Revised 02-Jun-08
Isoxanthohumol
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-279-M001   1 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C21H22O5
MW: 354.4
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: White powder.
SOLUBILITY: Soluble in DMSO (50mg/ml) or methanol (50mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Prenylated flavonoid. Phytoestrogen. Induces apoptosis in mature adipocytes.
Product Specific Literature References
Xanthohumol and related prenylflavonoids from hops and beer: to your good health!: J.F. Stevens & J.E. Page; Phytochemistry 65, 1317 (2004), (Review) Abstract
Inhibition of endothelial cell functions by novel potential cancer chemopreventive agents: E. Bertl, et al.; BBRC 325, 287 (2004) Abstract
Metabolism of xanthohumol and isoxanthohumol, prenylated flavonoids from hops (Humulus lupulus L.), by human liver microsomes: D. Nikolic, et al.; J. Mass Spectrom. 40, 289 (2005) Abstract
The prenylflavonoid isoxanthohumol from hops (Humulus lupulus L.) is activated into the potent phytoestrogen 8-prenylnaringenin in vitro and in the human intestine: S. Possemiers, et al.; J. Nutr. 136, 1862 (2006) Abstract
Identification of human hepatic cytochrome P450 enzymes involved in the metabolism of 8-prenylnaringenin and isoxanthohumol from hops (Humulus lupulus L.): J. Guo, et al.; Drug Metab. Dispos. 34, 1152 (2006)
Effect of xanthohumol and isoxanthohumol on 3T3-L1 cell apoptosis and adipogenesis: J.Y. Yang, et al.; Apoptosis 12, 1953 (2007) Abstract
Further Categories Containing This Product:
Flavanones • Estrogen & Estrogen Receptors / Related Products • Natural Products - Apoptosis Inducers & Inhibitors • Lipid Metabolism Other Products • Active Substances from Fruit and Vegetables • Natural Products - Other Signal Transduction Pathway Modulators
 
 
ALX-340-038 Revised 08-Sep-08
Leukotriene B4
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SYNONYMS LTB4
5,12-Dihydroxy-[S-[R*,S*-(E,Z,Z,E)]]-6,8,10,14-eicosatetraenoic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Leukotrienes
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ALX-340-038-C025   25 µg 170.00 USD Add To Cart
Product Specification
FORMULA: C20H32O4
MW: 336.5
CAS NUMBER: 71160-24-2
MERCK INDEX: 14: 5455
CONCENTRATION: 0.1mg/ml
PURITY: ≥97%
FORMULATION: Liquid. Solution in ethanol.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in PBS, pH 7.2 (1mg/ml). Solvents should be free of oxygen, transition metal ions, and redox active compounds.
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.