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Hormones & Hormone Receptors / Related Products
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ALX-270-204 Revised 11-Nov-08
bpV(phen)
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SYNONYMS Potassium bisperoxo (1,10-phenanthroline) oxovanadate (V)
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Oxovanadates
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ALX-270-204-M005   5 mg 53.00 USD Add To Cart
ALX-270-204-M025   25 mg 195.00 USD Add To Cart
Product Specification
FORMULA: K[VO(O2)2C12H8N2] . 3H2O
MW: 350.3 . 54.0
PURITY: ≥98% (51V-NMR)
APPEARANCE: Yellow to orange powder.
SOLUBILITY: Soluble in water (10mM).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
IDENTITY: Identity determined by 1H-NMR (D2O) and 51V-NMR (D2O)

Product Description
Potent protein phosphotyrosine phosphatase inhibitor. Also shown to be a potent insulin receptor kinase activator; excellent insulin mimetic in vitro and in vivo.
Product Specific Literature References
Peroxovanadium compounds. A new class of potent phosphotyrosine phosphatase inhibitors which are insulin mimetics: B.I. Posner, et al.; J. Biol. Chem. 269, 4596 (1994) Abstract; Full Text
Selective activation of the rat hepatic endosomal insulin receptor kinase. Role for the endosome in insulin signaling: A.P. Bevan, et al.; J. Biol. Chem. 270, 10784 (1995) Abstract; Full Text
In vivo insulin mimetic effects of pV compounds: role for tissue targeting in determining potency: A.P. Bevan, et al.; Am. J. Physiol. 268, E60 (1995) Abstract
Hypoglycemic effects of peroxovanadium compounds in Sprague-Dawley and diabetic BB rats: J.F. Yale, et al.; Diabetes 44, 1274 (1995) Abstract
A role for tyrosine phosphorylation in both activation and inhibition of the insulin receptor tyrosine kinase in vivo: P.G. Drake, et al.; Endocrinology 137, 4960 (1996) Abstract
Phosphatidylinositol 3'-kinase and p70s6k are required for insulin but not bisperoxovanadium 1,10-phenanthroline (bpV(phen)) inhibition of insulin-like growth factor binding protein gene expression. Evidence for MEK-independent activation of mitogen-activ: C.J. Band & B.I. Posner; J. Biol. Chem. 272, 138 (1997) Abstract; Full Text
Lipopolysaccharide down-regulates the leukotriene C4 synthase gene in the monocyte-like cell line, THP-1: K.J. Serio, et al.; J. Immunol. 170, 2121 (2003) Abstract; Full Text
Further Categories Containing This Product:
Insulin & Insulin Receptor / Related Products
 
 
ALX-270-212 Revised 26-Jan-07
Captopril
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SYNONYMS (2S)-1-(3-Mercapto-2-methylpropionyl)-L-proline
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Angiotensin Converting Enzyme [ACE] & ACE2 / Related Products
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ALX-270-212-G001   1 g 20.00 USD Add To Cart
ALX-270-212-G005   5 g 70.00 USD Add To Cart
Product Specification
FORMULA: C9H15NO3S
MW: 217.3
CAS NUMBER: 62571-86-2
MERCK INDEX: 14: 1774
RTECS: UY0550000
PURITY: ≥98% (Assay)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water, chloroform, dichloromethane or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: MAY BE TERATOGENIC. HARMFUL.

Product Description
First orally active angiotensin-converting enzyme (ACE) inhibitor. Reversible and competitive inhibitor of LTA4 hydrolase. Inhibits angiogenesis. Antihypotensive agent.
 
 
ALX-270-213 Revised 13-Dec-06
S-Nitrosocaptopril
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Angiotensin Converting Enzyme [ACE] & ACE2 / Related Products
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ALX-270-213-M010   10 mg 60.00 USD Add To Cart
ALX-270-213-M050   50 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C9H14N2O4S
MW: 246.3
PURITY: ≥98%
APPEARANCE: Red crystals.
SOLUBILITY: Soluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Angiotensin-converting enzyme (ACE) inhibitor. Inhibitor of platelet aggregation. Its activity may depend on the homolytic cleavage of the S-N bond under physiological conditions, yielding nitric oxide (NO) and the parent compound, captopril (Prod. No. ALX-270-212).
Product Specific Literature References
S-nitrosocaptopril. I. Molecular characterization and effects on the vasculature and on platelets: J. Loscalzo, et al.; J. Pharmacol. Exp. Ther. 249, 726 (1989) Abstract
S-nitrosocaptopril. II. Effects on vascular reactivity: J.P. Cooke, et al.; J. Pharmacol. Exp. Ther. 249, 730 (1989) Abstract
The hemodynamic effects of S-nitrosocaptopril in anesthetized dogs: J.E. Shaffer, et al.; J. Pharmacol. Exp. Ther. 256, 704 (1991) Abstract
Dual role of S-nitrosocaptopril as an inhibitor of angiotensin-converting enzyme and a nitroso group carrier: J.W. Park; BBRC 189, 206 (1992) Abstract
Differential inhibition of platelet aggregation and calcium mobilization by nitroglycerin and stabilized nitric oxide: M. Amano, et al.; J. Cardiovasc. Pharmacol. 24, 860 (1994) Abstract
Vasorelaxing effect of S-nitrosocaptopril on dog coronary arteries: no cross-tolerance with nitroglycerin: T. Matsumoto, et al.; J. Pharmacol. Exp. Ther. 275, 1247 (1995) Abstract
The effects of S-nitrosocaptopril on canine coronary circulation: I. Nakae, et al.; J. Pharmacol. Exp. Ther. 274, 40 (1995) Abstract
The effects of S-nitrosocaptopril on renal filtration and blood pressure in rats: L. Jia & R.C. Blantz; Eur. J. Pharmacol. 354, 33 (1998) Abstract
Physicochemistry, pharmacokinetics, and pharmacodynamics of S-nitrosocaptopril crystals, a new nitric oxide donor: L. Jia, et al.; J. Pharm. Sci. 88, 981 (1999) Abstract
Antiangiogenic effects of S-nitrosocaptopril crystals as a nitric oxide donor: L. Jia, et al.; Eur. J. Pharmacol. 391, 137 (2000) Abstract
In vitro and in vivo assessment of cellular permeability and pharmacodynamics of S-nitrosylated captopril, a nitric oxide donor: L. Jia & H. Wong; Br. J. Pharmacol. 134, 1697 (2001) Abstract
S-nitrosocaptopril: in vitro characterization of pulmonary vascular effects in rats: D.Y. Tsui, et al.; Br. J. Pharmacol. 138, 855 (2003) Abstract
S-nitrosocaptopril: acute in-vivo pulmonary vasodepressor effects in pulmonary hypertensive rats: D.Y. Tsui, et al.; J. Pharm. Pharmacol. 55, 1121 (2003) Abstract
 
 
ALX-270-312 Revised 03-Jan-08
Formononetin (high purity)
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SYNONYMS 7-Hydroxy-4’-methoxyisoflavone (high purity)
7-Hydroxy-3-(4’-methoxyphenyl)-4H-benzopyran-4-one (high purity)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Isoflavones
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ALX-270-312-M005   5 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C16H12O4
MW: 268.3
CAS NUMBER: 485-72-3
MERCK INDEX: 14: 4244
PURITY: ≥97%
APPEARANCE: White to greyish powder.
SOLUBILITY: Soluble in DMSO (200mg/ml) or methanol (2mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Place in a desiccator under vacuum for 48 hours before use.
HANDLING: Protect from light.

Product Description
Interacts with human estrogen receptors with low potency. Enhances IL-4 production in a dose-dependent manner. Inhibits lecithin peroxidation induced by hydroxyl radicals. Selective inhibitor of the γ-isoform of alcohol dehydrogenase. Antioxidant.
Product Specific Literature References
Interaction of naturally occurring nonsteroidal estrogens with expressed recombinant human estrogen receptor: R.J. Miksicek; J. Steroid Biochem. Mol. Biol. 49, 153 (1994) Abstract
Dietary estrogenic isoflavones are potent inhibitors of beta-hydroxysteroid dehydrogenase of P. testosteronii: W.M. Keung; BBRC 215, 1137 (1995) Abstract
Proliferative response of mammary glandular tissue to formononetin: W. Wang, et al.; Nutr. Cancer 23, 131 (1995) Abstract
Antioxidant activity of phytoestrogenic isoflavones: M.B. Ruiz-Larrea, et al.; Free Radic. Res. 26, 63 (1997) Abstract
Inhibitory effects of isoflavones on lipid peroxidation by reactive oxygen species: S. Toda and Y. Shirataki; Phytother. Res. 13, 163 (1999) Abstract
Isoflavonoids and lignans have different potentials to modulate oxidative genetic damage in human colon cells: B.L. Pool-Zobel, et al.; Carcinogenesis 21, 1247 (2000) Abstract
Disposition of flavonoids via enteric recycling: enzyme-transporter coupling affects metabolism of biochanin A and formononetin and excretion of their phase II conjugates: X. Jia, et al.; J. Pharmacol. Exp. Ther. 310, 1103 (2004) Abstract
Formononetin, a phyto-oestrogen, and its metabolites up-regulate interleukin-4 production in activated T cells via increased AP-1 DNA binding activity: J. Park, et al.; Immunology 116, 71 (2005) Abstract
 
 
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-270-476 Revised 11-Mar-08
Bicalutamide
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SYNONYMS N-(4-Cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methylpropanamide
PRODUCT LINE DNA Regulation / Transcription
PRODUCT CATEGORY Androgens & Androgen Receptors / Related Products
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-476-M100   100 mg 40.00 USD Add To Cart
ALX-270-476-M500   500 mg 140.00 USD Add To Cart
ALX-270-476-G001   1 g 220.00 USD Add To Cart
Product Specification
FORMULA: C18H14F4N2O4S
MW: 430.4
CAS NUMBER: 90357-06-5
SOURCE/HOST: Synthetic.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in acetone and tetrahydrofuran; slightly soluble in 100% ethanol or methanol; practically insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Nonsteroidal antiandrogen. Effective in the treatment of prostate cancer. Induces cell death by a pathway that is independent of changes in mitochondrial membrane potential and Bcl-2 action.
Product Specific Literature References
Antiproliferative activity of casodex (ICI 176.334) in hormone-dependent tumours: A. Maucher & E. von Angerer; J. Cancer Res. Clin. Oncol. 119, 669 (1993) Abstract
Antiandrogen-induced cell death in LNCaP human prostate cancer cells: E.C. Lee, et al.; Cell Death Differ. 10, 761 (2003) Abstract
Proanthocyanidins from grape seeds inhibit expression of matrix metalloproteinases in human prostate carcinoma cells, which is associated with the inhibition of activation of MAPK and NF kappa B: P.K. Vayalil, et al.; Carcinogenesis 25, 987 (2004) Abstract; Full Text
Wnt3a growth factor induces androgen receptor-mediated transcription and enhances cell growth in human prostate cancer cells: M. Verras, et al.; Cancer Res. 64, 8860 (2004) Abstract; Full Text
Glycogen synthase kinase-3beta activity is required for androgen-stimulated gene expression in prostate cancer: X. Liao, et al.; Endocrinology 145, 2941 (2004) Abstract; Full Text
A phase I pharmacokinetic and pharmacodynamic study of OGX-011, a 2’-methoxyethyl antisense oligonucleotide to clusterin, in patients with localized prostate cancer: K.N. Chi, et al.; J. Natl. Cancer Inst. 97, 1287 (2005) Abstract; Full Text
The mechanisms and managements of hormone-therapy resistance in breast and prostate cancers: K.M. Rau, et al.; Endocr. Relat. Cancer 12, 511 (2005), Review Abstract; Full Text
Signal transduction pathways in androgen-dependent and -independent prostate cancer cell proliferation: P.M. Ghosh, et al.; Endocr. Relat. Cancer 12, 119 (2005) Abstract; Full Text
Recent advances on multiple tumorigenic cascades involved in prostatic cancer progression and targeting therapies: M. Mimeault & S.K. Batra; Carcinogenesis 27, 1 (2006), Review Abstract; Full Text
Bcl-xL is overexpressed in hormone-resistant prostate cancer and promotes survival of LNCaP cells via interaction with proapoptotic Bak: C. Castilla, et al.; Endocrinology 147, 4960 (2006) Abstract; Full Text
Androgen receptor corepressors and prostate cancer: C.J. Burd, et al.; Endocr. Relat. Cancer 13, 979 (2006), Review Abstract; Full Text
Par-4-dependent apoptosis by the dietary compound withaferin A in prostate cancer cells: S. Srinivasan, et al.; Cancer Res. 67, 246 (2006) Abstract; Full Text
Androgen receptor structural and functional elements: role and regulation in prostate cancer: S.M. Dehm & D.J. Tindall; Mol. Endocrinol. 21, 2855 (2007), Review Abstract
Phosphoinositide 3-kinase-independent non-genomic signals transit from the androgen receptor to Akt1 in membrane raft microdomains: B. Cinar, et al.; JBC 282, 29584 (2007) Abstract; Full Text
A novel class of pyranocoumarin anti-androgen receptor signaling compounds: J. Guo, et al.; Mol. Cancer Ther. 6, 907 (2007) Abstract; Full Text
Increased resistance to trail-induced apoptosis in prostate cancer cells selected in the presence of bicalutamide: M. Mitterberger, et al.; Prostate 67, 1194 (2007) Abstract
Interplay of nuclear factor-kappaB and B-myb in the negative regulation of androgen receptor expression by tumor necrosis factor alpha: S. Ko, et al.; Mol. Endocrinol. 22, 273 (2008) Abstract
Further Categories Containing This Product:
Antitumor Agents (Hormone-related)Antitumor Agents (Apoptosis Inducers)
 
 
ALX-350-098 Revised 05-Apr-08
Ferutinin (high purity)
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SYNONYMS Tefestrol (high purity)
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Other Natural Products - DNA Regulation / Transcription
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ALX-350-098-M001   1 mg 35.00 USD Add To Cart
ALX-350-098-M005   5 mg 100.00 USD Add To Cart
ALX-350-098-M010   10 mg 170.00 USD Add To Cart
Product Specification
FORMULA: C22H30O4
MW: 358.5
SOURCE/HOST: Semisynthetic.
PURITY: ≥98%
SOLUBILITY: Soluble in acetone, dichloromethane, DMSO or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Potent, naturally occuring non-steroid estrogenic compound. Agonist for estrogen receptor (ER) α and agonist/antagonist for ERβ with higher binding affinity than tamoxifen (Prod. No. ALX-550-095) for both ERs. Electrogenic Ca2+ ionophore inducing mitochondrial depolarisation which can be completely blocked by cyclosporin A (Prod. No. ALX-380-002), suggesting that ferutinin opens the mitochondrial permeability transition pore (mPTP). In a concentration range of 1-50µM ferutinin increases the permeability of thymocytes, mitochondria, sarcoplasmic reticulum, liposomes and bilayer lipid membranes for Ca2+.
Product Specific Literature References
Ferutinine structure: A.I. Saidkhodjaev, et al.; Chem. Nat. Comp. 1, 28 (1973)
Ionophoretic properties of ferutinin: M.V. Zamaraeva, et al.; Cell Calcium 22, 235 (1997) Abstract
Influence of plant terpenoids on the permeability of mitochondria and lipid bilayers: A.Y. Abramov, et al.; Biochim. Biophys. Acta 1512, 98 (2001) Abstract
Daucane phytoestrogens: a structure-activity study: G. Appendino, et al.; J. Nat. Prod. 65, 1612 (2002) Abstract
Terpenoids found in the umbelliferae family act as agonists/antagonists for ER(alpha) and ERbeta: differential transcription activity between ferutinine-liganded ER(alpha) and ERbeta: K. Ikeda, et al.; BBRC 291, 354 (2002) Abstract
Actions of ionomycin, 4-BrA23187 and a novel electrogenic Ca2+ ionophore on mitochondria in intact cells: A.Y. Abramov & M.R. Duchen; Cell Calcium 33, 101 (2003) Abstract
 
 
ALX-350-147 Revised 03-Oct-07
Bavachin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-350-147-MC05   0.5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C20H20O4
MW: 324.4
CAS NUMBER: 19879-32-4
SOURCE/HOST: Isolated from plant Psoralea corylifolia.
PURITY: ≥97% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.
IDENTITY: Determined by 1H-NMR, 13C-NMR and MS.

Product Description
Weak antioxidant. Antimutagenic. Stimulates bone formation and has potential activity against osteoporosis. Shows inhibitory activities against the antigen-induced degranulation and weak estrogen-like activity.
Product Specific Literature References
Antiplatelet flavonoids from seeds of Psoralea corylifolia: W.J. Tsai, et al.; J. Nat. Prod. 59, 671 (1996) Abstract
Osteoblastic proliferation stimulating activity of Psoralea corylifolia extracts and two of its flavonoids: D. Wang, et al.; Planta Med. 67, 748 (2001) Abstract
Antioxidative components of Psoralea corylifolia (Leguminosae): H. Haraguchi, et al.; Phytother. Res. 16, 539 (2002) Abstract
Bioactive constituents from Chinese natural medicines. XX. Inhibitors of antigen-induced degranulation in RBL-2H3 cells from the seeds of Psoralea corylifolia: H. Matsuda, et al.; Chem. Pharm. Bull. (Tokyo) 55, 106 (2007) Abstract
Synthesis of four natural prenylflavonoids and their estrogen-like activities: X. Dong, et al.; Arch. Pharm. (Weinheim) 340, 372 (2007) Abstract
 
 
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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-279-M001   1 mg 60.00 USD