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COX Inhibitors
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Items 33 of 33
ALX-430-096 Revised 24-Feb-05
A77 1726
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SYNONYMS N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide
2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-430-096-M005   5 mg 45.00 USD Add To Cart
ALX-430-096-M025   25 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C12H9F3N2O2
MW: 270.2
CAS NUMBER: 108605-62-5
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. Keep under inert gas.

Product Description
Physiologically active metabolite of the immunosuppressive drug leflunomide (Prod. No. ALX-430-095). Inhibits the activity of dihydrorotate dehydrogenase and of protein tyrosine kinases. Blocks TNF-mediated NF-κB activation in a dose- and time-dependent manner. Also inhibits the activity of cyclooxygenase-2 (COX-2) in vitro and in vivo.
Product Specific Literature References
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide: T. Mattar, et al.; FEBS Lett. 334, 161 (1993) Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide: X. Xu, et al.; J. Biol. Chem. 270, 12398 (1995) Abstract; Full Text
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase: J.P. Davis, et al.; Biochemistry 35, 1270 (1996) Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation: X. Xu, et al.; Biochem. Pharmacol. 52, 527 (1996) Abstract
The immunosuppressive metabolite of leflunomide, A77 1726, affects murine T cells through two biochemical mechanisms: R.T. Elder, et al.; J. Immunol. 159, 22 (1997) Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice: X. Xu, et al.; J. Immunol. 159, 167 (1997) Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF-dependent nuclear factor-kappa B activation and gene expression: S.K. Manna & B.B. Aggarwal; J. Immunol. 162, 2095 (1999) Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate-sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999) Abstract
Further Categories Containing This Product:
Immunomodulators Other ProductsNF-kB Pathway InhibitorsCOX Inhibitors
 
 
ALX-430-115 Revised 14-Aug-08
Aspirin
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SYNONYMS Acetylsalicylic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-430-115-G005   5 g 10.00 USD Add To Cart
Product Specification
FORMULA: C9H8O4
MW: 180.2
CAS NUMBER: 50-78-2
MERCK INDEX: 14: 851
RTECS: VO0700000
PURITY: ≥99%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in 100% ethanol (80mg/ml), DMSO (41mg/ml) or dimethyl formamide (30mg/ml); slightly soluble in PBS, pH 7.2 (2.7mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Stable for at least 2 years when stored at room temperature. Keep aqueous solutions on ice and use within 30 minutes. Unstable in basic solutions pH>7.4.
HAZARD: HARMFUL.

Product Specific Literature References
Inhibition of NF-kappa B by sodium salicylate and aspirin: E. Kopp & S. Ghosh; Science 265, 956 (1994) Abstract
Neuroprotection by aspirin and sodium salicylate through blockade of NF- kappaB activation: M. Grilli, et al.; Science 274, 1383 (1996) Abstract
The anti-inflammatory agents aspirin and salicylate inhibit the activity of I(kappa)B kinase-beta: M.J. Yin, et al.; Nature 396, 77 (1998) Abstract
The pleiotropic functions of aspirin: mechanisms of action: A.R. Amin, et al.; Cell Mol. Life Sci. 56, 305 (1999) Abstract
 
 
ALX-270-254 Revised 22-Sep-08
Carnosol
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SYNONYMS 1,3,4,9,10,10aS-Hexahydro-5,6-dihydroxy-1,1-dimethyl-7-isopropyl-2H-9S,4aR-(epoxymethano)phenanthren-12-one
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Antioxidants
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ALX-270-254-M001   1 mg 60.00 USD Add To Cart
ALX-270-254-M005   5 mg 269.00 USD Add To Cart
Product Specification
FORMULA: C20H26O4
MW: 330.4
CAS NUMBER: 5957-80-2
SOURCE/HOST: Isolated from Rosmarinus officinalis.
PURITY: ≥96%
APPEARANCE: White to beige solid.
SOLUBILITY: Soluble in 100% ethanol (8mg/ml), DMSO (250mg/ml) or dimethyl formamide (35mg/ml); sparingly soluble in aqueous PBS, pH 7.2 (<30μg/ml).
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.
HANDLING: Protect from light.

Product Description
Naturally occurring phenolic compound with antioxidant and anti-inflammatory properties. Suppresses nitric oxide (NO) production and inducible nitric oxide synthase (iNOS; NOS II) gene expression by inhibiting NF-κB activation. Inhibits lipid peroxidation. Antimicrobial. Anticarcinogenic. Inhibits cyclooxygenase-2 (COX-2).
Product Specific Literature References
Antioxidant and pro-oxidant properties of active rosemary constituents: carnosol and carnosic acid: O.I. Aruoma, et al.; Xenobiotica 22, 257 (1992) Abstract
Effects of three dietary phytochemicals from tea, rosemary and turmeric on inflammation-induced nitrite production: M.M. Chan, et al.; Cancer Lett. 96, 23 (1995) Abstract
Inhibition of lipid peroxidation and superoxide generation by diterpenoids from Rosmarinus officinalis: H. Haraguchi, et al.; Planta Med. 61, 333 (1995) Abstract
Inhibition by rosemary and carnosol of 7,12-dimethylbenz[a]anthracene (DMBA)-induced rat mammary tumorigenesis and in vivo DMBA-DNA adduct formation: K. Singletary, et al.; Cancer Lett. 104, 43 (1996) Abstract
Development of in vitro models for cellular and molecular studies in toxicology and chemoprevention: K. Macé, et al.; Arch. Toxicol. Suppl. 20, 227 (1998) Abstract
Carnosol, an antioxidant in rosemary, suppresses inducible nitric oxide synthase through down-regulating nuclear factor-kappaB in mouse macrophages: A.H. Lo, et al.; Carcinogenesis 23, 983 (2002) 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
 
 
ALX-350-028 Revised 12-Sep-08
Curcumin (high purity)
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SYNONYMS 1,7-bis(4-Hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione
Diferuloylmethane
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Anti-inflammatory Agents
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ALX-350-028-M010   10 mg 15.00 USD Add To Cart
ALX-350-028-M050   50 mg 60.00 USD Add To Cart
ALX-350-028-M250   250 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C21H20O6
MW: 368.4
CAS NUMBER: 458-37-7
MERCK INDEX: 14: 2673
SOURCE/HOST: Isolated from turmeric (Curcuma longa).
PURITY: ≥98.5% (Note: This highly purified product is free of demethoxy- and bis-demethoxycurcumin and does not contain 30-40% bioactive impurities)
APPEARANCE: Orange-yellow crystalline powder.
SOLUBILITY: Soluble in acetic acid or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Protect from light.

Product Description
Dual inhibitor of cyclooxygenase (COX) and 5-lipoxygenase. Also inhibits glutathione S-transferase, induction of nitric oxide (NO) in activated macrophages and inhibits EGF-induced tyrosine phosphorylation of EGF receptors. Antioxidant. Inhibitor of NAD(P)H:quinone oxidoreductase 1 (NQO1), disrupting the binding of NQO1 to wild type p53 inducing ubiquitin-independent degradation of p53 and inhibits p53-mediated apoptosis in normal thymocytes and myeloid leukemic cells.
Product Specific Literature References
Modification of certain inflammation-induced biochemical changes by curcumin: R. Srivastava & R.C. Srimal; Indian J. Med. Res. 81, 215 (1985) Abstract
Inhibition of 5-hydroxy-eicosatetraenoic acid (5-HETE) formation in intact human neutrophils by naturally-occurring diarylheptanoids: inhibitory activities of curcuminoids and yakuchinones: D.L. Flynn, et al.; Prostagl. Leukotr. Med. 22, 357 (1986) Abstract
Inhibitory effect of curcumin on epidermal growth factor receptor kinase activity in A431 cells: L. Korutla & R. Kumar; Biochim. Biophys. Acta 1224, 597 (1994) Abstract
Curcumin, an anti-tumour promoter and anti-inflammatory agent, inhibits induction of nitric oxide synthase in activated macrophages: I. Brouet & H. Okshima; BBRC 206, 533 (1995) Abstract
Cytotoxicity and cytoprotective activities of natural compounds. The case of curcumin: J.N. Commandeur & N.P. Vermeulen; Xenobiotica 26, 667 (1996) Abstract
Nitric oxide scavenging by curcuminoids: Sreejayan & M.N. Rao; J. Pharm. Pharmacol. 49, 105 (1997) Abstract
Inhibitory effects of curcumin on tumorigenesis in mice: M.T. Huang, et al.; J. Cell. Biochem. (Suppl.) 27, 26 (1997) Abstract
In vivo inhibition of nitric oxide synthase gene expression by curcumin, a cancer preventive natural product with anti-inflammatory properties: M.M. Chan, et al.; Biochem. Pharmacol. 55, 1955 (1998) Abstract
Effect of curcumin on the production of nitric oxide by cultured rat mammary gland: M. Onoda & H. Inano; Nitric Oxide 4, 505 (2000) Abstract
Suppression of nitric oxide oxidation to nitrite by curcumin is due to the sequestration of the reaction intermediate nitrogen dioxide, not nitric oxide: B.D. Johnston & E.G. DeMaster; Nitric Oxide 8, 231 (2003) Abstract
Biological properties of curcumin-cellular and molecular mechanisms of action: B. Joe, et al.; Crit. Rev. Food Sci. Nutr. 44, 97 (2004), (Review) Abstract
Curcumin, a major constituent of turmeric, corrects cystic fibrosis defects: M.E. Egan, et al.; Science 304, 600 (2004) Abstract
Inhibition of NAD(P)H:quinone oxidoreductase 1 activity and induction of p53 degradation by the natural phenolic compound curcumin: P. Tsvetkov, et al.; PNAS 102, 5535 (2005) Abstract
Immunomodulatory effects of curcumin: V.S. Yadav, et al.; Immunopharmacol. Immunotoxicol. 27, 485 (2005) Abstract
Curcumin, an atoxic antioxidant and natural NFkappaB, cyclooxygenase-2, lipooxygenase, and inducible nitric oxide synthase inhibitor: a shield against acute and chronic diseases: S. Bengmark; JPEN J. Parenter. Enteral. Nutr. 30, 45 (2006), (Review) Abstract
Curcumin is an inhibitor of p300 histone acetylatransferase: M.G. Marcu, et al.; Med. Chem. 2, 169 (2006) Abstract
Multiple biological activities of curcumin: a short review: R.K. Maheshwari, et al.; Life Sci. 78, 2081 (2006), (Review) Abstract
Curcumin inhibits hypoxia-induced angiogenesis via down-regulation of HIF-1: M.K. Bae, et al.; Oncol. Rep. 15, 1557 (2006) Abstract
Notch-1 down-regulation by curcumin is associated with the inhibition of cell growth and the induction of apoptosis in pancreatic cancer cells: Z. Wang, et al.; Cancer 106, 2503 (2006) Abstract
Curcumin improves wound healing by modulating collagen and decreasing reactive oxygen species: M. Panchatcharam, et al.; Mol. Cell Biochem. 290, 87 (2006) Abstract
Inhibitory effect of curcumin on nitric oxide production from lipopolysaccharide-activated primary microglia: K.K. Jung, et al.; Life Sci. 79, 2022 (2006) Abstract
The dietary compound curcumin inhibits p300 histone acetyltransferase activity and prevents heart failure in rats: T. Morimoto, et al.; J. Clin. Invest. 118, 868 (2008) Abstract; Full Text
 
 
ALX-350-118 Revised 22-Sep-08
Deguelin
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SYNONYMS [-]-Deguelin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-118-M005   5 mg 60.00 USD Add To Cart
ALX-350-118-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C23H22O6
MW: 394.4
CAS NUMBER: 522-17-8
MERCK INDEX: 14: 2863
RTECS: DX1500000
PURITY: ≥95%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in acetone, acetonitrile or DMSO. Slightly soluble in 100% ethanol. Insoluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Inhibitor of Akt (protein kinase B; PKB) in an in vitro lung carcinogenesis progression model. Inhibits cell proliferation - cells accumulate in the G2-M phase of the cell cycle. Induces apoptosis. Exhibits a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. Inhibits cyclooxygenase-2 (COX-2) expression.
Product Specific Literature References
Deguelin inhibits the growth of colon cancer cells through the induction of apoptosis and cell cycle arrest: G. Murillo, et al.; Eur. J. Cancer 38, 2446 (2002) Abstract
Effects of deguelin on the phosphatidylinositol 3-kinase/Akt pathway and apoptosis in premalignant human bronchial epithelial cells: K.H. Chun, et al.; J. Natl. Cancer Inst. 95, 291 (2003) Abstract; Full Text
Cancer Chemopreventive Activity of Rotenoids from Derris trifoliata: C. Ito, et al.; Planta Med. 70, 8 (2004) Abstract
Apoptosis induction by the natural product cancer chemopreventive agent deguelin is mediated through the inhibition of mitochondrial bioenergetics.: N. Hail, et al.; Apoptosis 9, 437 (2004) Abstract
Deguelin-induced inhibition of cyclooxygenase-2 expression in human bronchial epithelial cells: H.Y. Lee, et al.; Clin. Cancer Res. 10, 1074 (2004) Abstract
 
 
ALX-270-097 Revised 07-Sep-06
Ebselen
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SYNONYMS 2-Phenyl-1,2-benzisoselenazol-3-(2H)-one
PRODUCT LINE Oxidative Stress
PRODUCT CATEGORY Peroxynitrite / Scavengers / Detection
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ALX-270-097-M001   1 mg 12.00 USD Add To Cart
ALX-270-097-M005   5 mg 20.00 USD Add To Cart
ALX-270-097-M025   25 mg 60.00 USD Add To Cart
Product Specification
FORMULA: C13H9NOSe
MW: 274.2
CAS NUMBER: 60940-34-3
PURITY: ≥98% (NMR)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Selenium-based inhibitor of protein kinase C, NADPH, 5-lipoxygenase, cyclooxygenase (COX) and NADPH oxidase. Anti-inflammatory antioxidant. Mimics glutathione peroxidase. Inhibits oxidative modifications of low density lipoproteins (LDL).
Product Specific Literature References
A novel biologically active seleno-organic compound--III. Effects of PZ 51 (Ebselen) on glutathione peroxidase and secretory activities of mouse macrophages: M.J. Parnham & S. Kindt; Biochem. Pharmacol. 33, 3247 (1984) Abstract
Seleno-organic compounds and the therapy of hydroperoxide-linked pathological conditions: M.J. Parnham & E. Graf; Biochem. Pharmacol. 36, 3095 (1987) Abstract
Kinetic mechanism and substrate specificity of glutathione peroxidase activity of ebselen (PZ51): M. Maiorino, et al.; Biochem. Pharmacol. 37, 2267 (1988) Abstract
Studies on the anti-inflammatory activity of ebselen. Ebselen interferes with granulocyte oxidative burst by dual inhibition of NADPH oxidase and protein kinase C?: I.A. Cotgreave, et al.; Biochem. Pharmacol. 38, 649 (1989) Abstract
T. Nikawa, et al.; Biochem. Pharmacol. 47, 1007 (1994) Abstract
Effects of ebselen and probucol on oxidative modifications of lipid and protein of low density lipoprotein induced by free radicals: N. Noguchi, et al.; Biochim. Biophys. Acta 1213, 176 (1994) Abstract
Strong inhibition of mammalian lipoxygenases by the antiinflammatory seleno-organic compound ebselen in the absence of glutathione: C. Schewe, et al.; Biochem. Pharmacol. 48, 65 (1994) Abstract
Ebselen: a glutathione peroxidase mimic: H. Sies; Meth. Enzymol. 234, 476 (1994) Abstract
Molecular actions of ebselen-an antiinflammatory antioxidant: T. Schewe; Gen. Pharmacol. 26, 1153 (1995) Abstract
Ebselen: H. Sies; Meth. Enzymol. 252, 341 (1995) Abstract
Ebselen as a glutathione peroxidase mimic and as a scavenger of peroxynitrite: H. Sies & H. Masumoto; Adv. Pharmacol. 38, 229 (1997) Abstract
Free radical generation by selenium compounds and their prooxidant toxicity: J.E. Spallholz; Biomed. Environ. Sci. 10, 260 (1997) Abstract
Protection against peroxynitrite by selenoproteins: H. Sies, et al.; Z. Naturforsch. [C] 53, 228 (1998) Abstract
Ebselen protects mice against T cell-dependent, TNF-mediated apoptotic liver injury: G. Tiegs, et al.; J. Pharmacol. Exp. Ther. 287, 1098 (1998) Abstract; Full Text
 
 
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
 
 
ALX-550-249 Revised 27-May-03
Ibuprofen
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SYNONYMS α-Methyl-4-(2-methylpropyl)benzeneacetic acid
(±)-2-(4-Isobutylphenyl)propionic acid
PRODUCT LINE Inflammation
PRODUCT CATEGORY Non-Steroidal Anti-Inflammatory Drugs [NSAIDS]
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ALX-550-249-G001   1 g 17.00 USD Add To Cart
ALX-550-249-G005   5 g 48.00 USD Add To Cart
Product Specification