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ALX-420-029
Revised 22-Feb-08
GW1929
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
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-420-029-M001
1 mg
80.00 USD
ALX-420-029-M005
5 mg
360.00 USD
Product Specification
FORMULA:
C
30
H
29
N
3
O
4
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
SYNONYMS
2-Chloro-5-nitrobenzanilide
PRODUCT LINE
DNA Regulation / Transcription
PRODUCT CATEGORY
PPAR Antagonists
Ordering Information
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Format:
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ALX-270-356-M001
1 mg
10.00 USD
ALX-270-356-M005
5 mg
35.00 USD
ALX-270-356-M025
25 mg
140.00 USD
Product Specification
FORMULA:
C
13
H
9
N
2
O
3
Cl
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 06-Aug-07
GW501516
PRODUCT LINE
DNA Regulation / Transcription
PRODUCT CATEGORY
PPAR Agonists
Ordering Information
Product Numbers:
Format:
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ALX-420-032-M001
1 mg
83.00 USD
ALX-420-032-M005
5 mg
367.00 USD
Product Specification
FORMULA:
C
21
H
18
F
3
NO
3
S
2
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 (EC
50
=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-350-371
Revised 10-Mar-08
Harmine
SYNONYMS
Leucoharmine
Banisterine
Telepathine
Yageine
7-Methoxy-1-methyl-
9H
-pyrido[3,4-
b
]indole
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Other Natural Products - DNA Regulation/Transcription
Ordering Information
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Format:
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ALX-350-371-M250
250 mg
22.00 USD
Product Specification
FORMULA:
C
13
H
12
N
2
O
MW:
212.3
CAS NUMBER:
442-51-3
MERCK INDEX:
14:
4616
RTECS:
UV0175000
SOURCE/HOST:
Originally isolated from
Peganum harmala
.
PURITY:
≥98%
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO, dimethyl formamide or 100% ethanol; slightly soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HAZARD:
HARMFUL.
Product Description
Alkaloid of the β-carboline family. Regulates PPARγ expression. Inhibits the Wnt signalling pathway in a cell-specific manner. Down-regulates inflammatory gene expression (TNF-α, IL-1β, iNOS). Reversibly inhibits monoamine oxidase inhibitor A (MAO-A), but has no effect on MAO-B.
Product Specific Literature References
The chemotherapy of derivatives of harmine and harmaline. I:
C.E. Coulthard, et al.; Biochee. J.
27
, 727 (1933)
Abstract
;
Full Text
The chemotherapy of derivatives of harmine and harmaline. II:
C.E. Coulthard; Biochem. J.
28
, 264 (1934)
Abstract
;
Full Text
Interrelationships between amphetamine and harmala alkaloids:
H. Schmitt; Nature
203
, 877 (1964)
Abstract
Effect of moclobemide on rat brain monoamine oxidase A and B: comparison with harmaline and clorgyline:
J. Gerardy; Prog. Neuropsychopharmacol. Biol. Psychiatry
18
, 793 (1994)
Abstract
Hypothermic effect of harmala alkaloid in rats: involvement of serotonergic mechanism:
A.F. Abdel-Fattah, et al.; Pharmacol. Biochem. Behav.
52
, 421 (1995)
Abstract
The mode of action of thiazolidinediones:
H. Hauner; Diabet. Metab. Res. Rev.
18
, S10 (2002)
Abstract
Antitumor and neurotoxic effects of novel harmine derivatives and structure-activity relationship analysis:
Q. Chen, et al.; Int. J. Cancer
114
, 675 (2005)
Abstract
The small molecule harmine is an antidiabetic cell-type-specific regulator of PPARgamma expression:
H. Waki, et al.; Cell Metab.
5
, 357 (2007)
Abstract
Further Categories Containing This Product:
Natural Products - Other Signal Transduction Pathway Modulators
•
Antidiabetic Agents/Related Products
•
Interleukin-1 [IL-1] & Receptors/Related Products
•
Wnt Signalling Pathway Other Products
•
TNF-alpha & TNF Receptors Other Products
•
NOS Regulation
•
Alkaloids
ALX-340-037
Revised 08-Jul-08
8(S)-HETE
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
Product Specification
FORMULA:
C
20
H
32
O
3
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 Na
2
CO
3
(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-300-131
Revised 04-Feb-05
2-Hydroxymyristic acid
SYNONYMS
2-Hydroxy-tetradecanoic acid
PRODUCT LINE
Obesity & Adipokines
PRODUCT CATEGORY
Fatty Acids
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ALX-300-131-M025
25 mg
35.00 USD
Product Specification
FORMULA:
C
14
H
28
O
3
MW:
244.4
CAS NUMBER:
2507-55-3
PURITY:
≥97%
APPEARANCE:
White solid.
SOLUBILITY:
Soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Selective inhibitor of protein myristoylation in cells, able to distinguish myristoylation from palmitoylation. Metabolic activation appears to be required. Myristoylation takes place on glycine residues at the N-terminus of proteins and provides a strong membrane anchor for the modified proteins, many of which require myristoylation for full activity.
Product Specific Literature References
Activation of p56lck through mutation of a regulatory carboxy-terminal tyrosine residue requires intact sites of autophosphorylation and myristylation:
N. Abraham & A. Veillette; Mol. Cell. Biol.
10
, 5197 (1990)
Abstract
Metabolic activation of 2-substituted derivatives of myristic acid to form potent inhibitors of myristoyl CoA:protein N-myristoyltransferase:
L.A. Paige, et al.; Biochemistry
29
, 10566 (1990)
Abstract
The G protein connection: molecular basis of membrane association [published erratum appears in TIBS 17, 177 (1992)]:
A.M. Spiegel, et al.; TIBS
16
, 338 (1991), (Review)
Abstract
Treatment of T cells with 2-hydroxymyristic acid inhibits the myristoylation and alters the stability of p56lck:
M.J.S. Nadler, et al.; Biochemistry
32
, 9250 (1993)
Abstract
Reversible palmitoylation of the protein-tyrosine kinase p56lck:
L.A. Paige, et al.; J. Biol. Chem.
268
, 8669 (1993)
Abstract
;
Full Text
Inhibition of varicella-zoster virus replication by an inhibitor of protein myristoylation:
D.R. Harper, et al.; J. Gen. Virol.
74
, 1181 (1993)
Abstract
ALX-582-001
Revised 02-Jul-08
Isopropyl-β-D-thiogalactoside (analytical grade, free of dioxane)
SYNONYMS
IPTG (analytical grade, free of dioxane)
PRODUCT LINE
Obesity & Adipokines
PRODUCT CATEGORY
Carbohydrates
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ALX-582-001-G001
1 g
33.00 USD
ALX-582-001-G005
5 g
85.00 USD
ALX-582-001-G025
25 g
290.00 USD
Product Specification
FORMULA:
C
9
H
18
O
5
S
MW:
238.3
CAS NUMBER:
367-93-1
PURITY:
≥98% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water (5%).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
ALX-350-279
Revised 02-Jun-08
Isoxanthohumol
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Other Natural Products - DNA Regulation/Transcription
Ordering Information
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ALX-350-279-M001
1 mg
60.00 USD
Product Specification
FORMULA:
C
21
H
22
O
5
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:
Natural Products - Other Signal Transduction Pathway Modulators
•
Estrogen & Estrogen Receptors/Related Products
•
Natural Products - Apoptosis Inducers & Inhibitors
•
Active Substances from Fruit and Vegetables
•
Lipid Metabolism Other Products
•
Flavonoids/Related Products
ALX-270-236
Revised 04-Feb-05
JM 34
SYNONYMS
N-(4,6-Dimethylpyridin-2-yl)furane-2-carboxamide
PRODUCT LINE
Chemokines & Cytokines
PRODUCT CATEGORY
TNF-alpha & TNF Receptors Other Products
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ALX-270-236-M010
10 mg
60.00 USD
Product Specification
FORMULA:
C
12
H
12
N
2
O
2
MW:
216.2
PURITY:
≥99%
APPEARANCE:
White solid.
SOLUBILITY:
Soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
USE/STABILITY:
For biological studies, solubilize as a maleate salt just before use.
HANDLING:
Keep under inert gas. Protect from light.
Product Description
Anti-inflammatory pyridinylamide that inhibits TNF-α production, probably by interacting with a protein kinase C (PKC)-dependent pathway of ERK2 phosphorylation. No inhibition of PKC activity
in vitro
. May serve as an alternative to classical cyclooxygenase (COX) inhibitors in TNF-α pathogenesis.
Product Specific Literature References
New antiinflammatory compounds that inhibit tumor necrosis factor production: probable interaction with protein kinase C activation:
F. Lang, et al.; J. Pharmacol. Exp. Ther.
275
, 171 (1995)
Abstract
An anti-inflammatory benzamide derivative inhibits the protein kinase C (PKC)-dependent pathway of ERK2 phosphorylation in murine macrophages:
L. Vernhet, et al.; J. Pharmacol. Exp. Ther.
283
, 358 (1997)
Abstract
;
Full Text
ALX-270-235
Revised 04-Feb-05
JM 42
SYNONYMS
N-(4,6-Dimethylpyridin-2-yl)-5-bromofurane-2-carboxamide
PRODUCT LINE
Chemokines & Cytokines
PRODUCT CATEGORY
TNF-alpha & TNF Receptors Other Products
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