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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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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
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 with Antibiotic Activity • Neuroactive Agents Other Products • Antitumor Agents (Apoptosis Inducers) • Natural Products - Apoptosis Inducers & Inhibitors • Natural Products - Antitumor Reagents
 
 
ALX-350-030 Revised 20-Oct-08
Hypericin (native)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Protein Kinase Inhibitors
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-350-030-M001   1 mg 50.00 USD Add To Cart
ALX-350-030-M005   5 mg 200.00 USD Add To Cart
ALX-350-030-M010   10 mg 370.00 USD Add To Cart
Product Specification
FORMULA: C30H16O8
MW: 504.4
CAS NUMBER: 548-04-9
MERCK INDEX: 14: 4863
SOURCE/HOST: Isolated from Hypericum perforatum.
PURITY: ≥98% (HPLC)
APPEARANCE: Black to black-red powder.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol, acetone, ethylmethylketone, pyridine or other organic solvents and bases.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light and oxygen.
HAZARD: MAY BE TERATOGENIC. HARMFUL. MAY BE MUTAGENIC.

Product Description
Inhibitor of protein kinase C (PKC). Shows anti-viral and anti-retroviral activity. Displays antineoplastic and antitumor activities. Inhibits casein kinase II (CKII) and MAP kinase. Bright red fluorescence emission and photostability. Antidepressant.
Product Specific Literature References
Therapeutic agents with dramatic antiretroviral activity and little toxicity at effective doses: aromatic polycyclic diones hypericin and pseudohypericin: D. Meruelo, et al.; PNAS 85, 5230 (1988) Abstract
Hypericin and pseudohypericin specifically inhibit protein kinase C: possible relation to their antiretroviral activity: I. Takahashi, et al.; BBRC 165, 1207 (1989) Abstract
Evaluation of the antiviral activity of anthraquinones, anthrones and anthraquinone derivatives against human cytomegalovirus: D.L. Barnard, et al.; Antiviral Res. 17, 63 (1992) Abstract
Photosensitized inhibition of growth factor-regulated protein kinases by hypericin: P. Agostinis, et al.; Biochem. Pharmacol. 49, 1615 (1995) Abstract
Growth inhibition and apoptosis in human neuroblastoma SK-N-SH cells induced by hypericin, a potent inhibitor of protein kinase C: W. Zhang, et al.; Cancer Lett. 96, 31 (1995) Abstract
Hypericin-induced photosensitization of HeLa cells leads to apoptosis or necrosis. Involvement of cytochrome c and procaspase-3 activation in the mechanism of apoptosis: A. Vantieghem, et al.; FEBS Lett. 440, 19 (1998) Abstract
The activation of the c-Jun N-terminal kinase and p38 mitogen-activated protein kinase signaling pathways protects HeLa cells from apoptosis following photodynamic therapy with hypericin: Z. Assefa, et al.; J. Biol. Chem. 274, 8788 (1999) Abstract; Full Text
Over-expression of Bcl-2 does not protect cells from hypericin photo- induced mitochondrial membrane depolarization, but delays subsequent events in the apoptotic pathway: R. Chaloupka, et al.; FEBS Lett. 462, 295 (1999) Abstract
Hypericin induces both differentiation and apoptosis in human promyelocytic leukemia HL-60 cells: K.T. Lee, et al.; Biol. Pharm. Bull. 22, 1271 (1999) Abstract
Apoptotic and anti-apoptotic signaling pathways induced by photodynamic therapy with hypericin: P. Agostinis, et al.; Adv. Enzyme Regul. 40, 157 (2000) Abstract
Hypericin--a new antiviral and antitumor photosensitizer: mechanism of action and interaction with biological macromolecules: P. Miskovsky; Curr. Drug Targets 3, 55 (2002), (Review) Abstract
Hypericin--the facts about a controversial agent: A. Kubin, et al.; Curr. Pharm. Des. 11, 233 (2005), (Review) Abstract
Cellular mechanisms and prospective applications of hypericin in photodynamic therapy: T. Kiesslich, et al.; Curr. Med. Chem. 13, 2189 (2006), (Review) Abstract
Further Categories Containing This Product:
Casein Kinase Inhibitors • MAPK Pathway Inhibitors • PKC Inhibitors • Neuroactive Agents Other Products • Natural Products for Neurological Research • Natural Products - Antiviral / anti-HIV Agents • Natural Products - Antitumor Reagents
 
 
ALX-380-116 Revised 07-Apr-08
Hypothemycin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Antifungal
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ALX-380-116-C250   250 µg 140.00 USD Add To Cart
ALX-380-116-M001   1 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C19H22O8
MW: 378.4
CAS NUMBER: 76958-67-3
SOURCE/HOST: Isolated from Phoma sp.
PURITY: ≥98% (HPLC)
APPEARANCE: Off-white solid.
SOLUBILITY: Soluble in DMSO or acetone; insoluble in methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Exhibits antifungal and cytotoxic activity against some tumor cell lines partly attributed to inhibition of Ras-inducible genes. Inhibits proliferation of mouse and human T cells and modulates production of cytokines during T cell activation. Facilitates the ubiquitinylation process of cyclin D1. Has been identified as a potent and selective inhibitor of threonine/tyrosine-specific kinase, MEK, and other protein kinases that contain a conserved cysteine residue in the ATP-binding site in both in vitro and in vivo studies.
Product Specific Literature References
Metabolites of pyrenomycetes XIII: Structure of (+) hypothemycin, an antibiotic macrolide from hypomyces trichothecoides: M.S.R. Nair & S.T. Carey; Tetrahedron Lett. 21, 2011 (1980)
Metabolites of pyrenomycetes. XIV: Structure and partial stereochemistry of the antibiotic macrolides hypothemycin and dihydrohypothemycin: M.S.R. Nair, et al.; Tetrahedron 37, 2445 (1981)
Revised structure and stereochemistry of hypothemycin: T. Agatsuma et al.; Chem. Pharm. Bull. 41, 373 (1993)
Antitumor efficacy of hypothemycin, a new Ras-signaling inhibitor: H. Tanaka, et al.; Jpn. J. Cancer Res. 90, 1139 (1999) Abstract
Hypothemycin inhibits the proliferative response and modulates the production of cytokines during T cell activation: R. Camacho, et al.; Immunopharmacology 44, 255 (1999) Abstract
Suppression of oncogenic transformation by hypothemycin associated with accelerated cyclin D1 degradation through ubiquitin-proteasome pathway: H. Sonoda, et al.; Life Sci. 65, 381 (1999) Abstract
Resorcylic acid lactones: naturally occurring potent and selective inhibitors of MEK: A. Zhao, et al.; J. Antibiot. 52, 1086 (1999) Abstract
Targeted covalent inactivation of protein kinases by resorcylic acid lactone polyketides: A. Schirmer, et al.; PNAS 103, 4234 (2006) Abstract; Full Text
Chemistry and biology of resorcylic acid lactones: N. Winssinger, et al.; Chem. Commun. (Camb). 1, 22 (2007), (Review) Abstract
Further Categories Containing This Product:
MAPK Pathway Inhibitors • Antibiotics - Protein Kinase Inhibitors • Tyrosine Kinase Inhibitors • Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Antibiotics • Antibiotics - Proteasome / Ubiquitin Modulators • Ubiquitination Other Products • CDKs & Cyclins Other Products • Ras Signalling Pathway Other Products
 
 
ALX-380-260 Revised 07-Apr-08
Idarubicin . hydrochloride
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SYNONYMS Idamycin
DMDR
4-Demethoxydaunorubicin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-380-260-M001   1 mg 45.00 USD Add To Cart
ALX-380-260-M005   5 mg 180.00 USD Add To Cart
Product Specification
FORMULA: C26H27NO9 . HCl
MW: 497.5 . 36.5
CAS NUMBER: 57852-57-0
MERCK INDEX: 14: 4886
RTECS: HB7877000
SOURCE/HOST: Synthetic.
PURITY: ≥98%
APPEARANCE: Orange crystalline solid.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC. MAY BE TERATOGENIC. MAY BE CARCINOGENIC.

Product Description
More potent, lipophilic and antineoplastic analog of daunorubicin. DNA-damaging effect includes DNA oxidation and methylation, DNA intercalation, inhibition of DNA synthesis, induction of DNA strand breaks and delay of cell cycle progression. Inhibitor of topoisomerase IIα. Produces endonucleolytic cleavage and is a marker of apoptosis.
Product Specific Literature References
Idarubicin (4-demethoxydaunorubicin). A preliminary overview of preclinical and clinical studies: F. Ganzina, et al.; Invest. New Drugs 4, 85 (1986), Review Abstract
Antitumor activity of idarubicin, a derivative of daunorubicin, against drug sensitive and resistant P388 leukemia: T. Tsuruo, et al.; Anticancer Res. 13, 357 (1993) Abstract
Study of apoptosis-related responses of leukemic blast cells to in vitro anthracycline treatment: M.A. Belaud-Rotureau, et al.; Leukemia 14, 1266 (2000) Abstract
A comparison of the in vitro genotoxicity of anticancer drugs idarubicin and mitoxantrone: J. Blasiak, et al.; Acta Biochim. Pol. 49, 145 (2002) Abstract; Full Text
Repair of idarubicin-induced DNA damage: A cause of resistance?: D.C. Dartsch & F. Gieseler; DNA Repair (Amst) 6, 1618 (2007) Abstract
Further Categories Containing This Product:
Antitumor Agents (DNA Interaction & Gene Regulation) • Antitumor Agents (Apoptosis Inducers) • Antibiotics - Topoisomerase Inhibitors • Antitumor Antibiotics
 
 
ALX-350-240 Revised 05-Dec-07
Ilimaquinone
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SYNONYMS 3-[(Decahydro-1β,2β,4αβ-trimethyl-5-methylene-1-naphthyl)methyl]-2-hydroxy-5-methoxybenzoquinone
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Other Signal Transduction Pathway Modulators
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ALX-350-240-C100   100 µg 140.00 USD Add To Cart
Product Specification
FORMULA: C22H30O4
MW: 358.5
CAS NUMBER: 71678-03-0
PURITY: ≥98%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Displays antimicrobial, anti-HIV and anti-inflammatory properties. Induces reversible breakdown of Golgi membranes. Inhibits the association of β-COP and ADP-ribosylation factor to Golgi membranes. Interacts with methylation enzymes. Shows anticancer activity.
Product Specific Literature References
R.T. Luibrand, et al.; Tetrahedron 35, 609 (1979)
Complete vesiculation of Golgi membranes and inhibition of protein transport by a novel sea sponge metabolite, ilimaquinone: P.A. Takizawa, et al.; Cell 73, 1079 (1993) Abstract
Interactions of (-)-ilimaquinone with methylation enzymes: implications for vesicular-mediated secretion: H.S. Radeke, et al.; Chem. Biol. 6, 639 (1999) Abstract
Ilimaquinone inhibits gap-junctional communication prior to Golgi fragmentation and block in protein transport: V. Cruciani, et al.; Exp. Cell Res. 287, 130 (2003) Abstract
Natural products with anti-HIV activity from marine organisms: L.A. Tziveleka, et al.; Curr. Top. Med. Chem. 3, 1512 (2003), Review Abstract
Interaction of the smooth endoplasmic reticulum and mitochondria: J.G. Goetz & I.R. Nabi; Biochem. Soc. Trans. 34, 370 (2006), Review Abstract
Ilimaquinone, a marine sponge metabolite, displays anticancer activity via GADD153-mediated pathway: P.H. Lu, et al.; Eur. J. Pharmacol. 556, 45 (2007) Abstract
Further Categories Containing This Product:
Natural Products - Anti-inflammatory Agents • Golgi Apparatus • ADP Ribosylation Factor [ARF] / Related Products • Natural Products - Chemopreventive Agents • Natural Products - Antiviral / anti-HIV Agents • PRMTs, Mono- & Dimethylarginine / Related Products • Marine Natural Products
 
 
ALX-350-302 Revised 14-Dec-07
Imperatorin
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Natural Products - Apoptosis Inducers & Inhibitors
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ALX-350-302-M002   2 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C16H14O4
MW: 270.3
PURITY: ≥99% (HPLC)
APPEARANCE: White to off-white crystalline solid.
SOLUBILITY: Soluble in DMSO or dimethyl formamide; slightly soluble in methanol or water. Almonst insoluble in 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
The furanocoumarins heraclenin (Prod. No. ALX-350-303) and imperatorin (Prod. No. ALX-350-302) inhibit T cell-receptor-mediated proliferation in human primary T cells in a concentration-dependent manner. Both compounds also induce apoptosis. While imperatorin induces DNA fragmentation at the G1/S phase of the cell cycle, heraclenin induces DNA fragmentation at the G2/M phases of the cell cycle, thus despite a close structural similarity they induce apoptosis in mechanistically different ways. Imperatorin inhibits HIV-1 replication as well as the expression of ICAM-1 in U937 foam cells. Inhibits voltage-dependent calcium channel.
Product Specific Literature References
Expression of intercellular adhesion molecule-1 in U937 foam cells and inhibitory effect of imperatorin: P.Y. Yang, et al.; Acta Pharmacol. Sin. 23, 327 (2002) Abstract
Imperatorin, a furanocoumarin from Angelica dahurica (Umbelliferae), induces cytochrome c-dependent apoptosis in human promyelocytic leukaemia, HL-60 Cells: H.O. Pae, et al.; Pharmacol. Toxicol. 91, 40 (2002) Abstract
Coumarins from Opopanax chironium. New dihydrofuranocoumarins and differential induction of apoptosis by imperatorin and heraclenin: G. Appendino, et al.; J. Nat. Prod. 67, 532 (2004) Abstract
Imperatorin inhibits T-cell proliferation by targeting the transcription factor NFAT: N. Marquez, et al.; Planta Med. 70, 1016 (2004) Abstract
Imperatorin inhibits HIV-1 replication through an Sp1-dependent pathway: R. Sancho, et al.; J. Biol. Chem. 279, 37349 (2004) Abstract; Full Text
Imperatorin induces vasodilatation possibly via inhibiting voltage dependent calcium channel and receptor-mediated Ca2+ influx and release: J.Y. He, et al.; Eur. J. Pharmacol. 573, 170 (2007) Abstract
Related Products
Further Categories Containing This Product:
DNA Fragmentation & Chromatin Condensation • Natural Products - Antiviral / anti-HIV Agents • CD11a, CD18 [LFA-1] & CD54 [ICAM-1], CD102 [ICAM-2], CD50 [ICAM-3] / Related Products • Ca2+ Channels Other Products • HIV / AIDS / Related Products
 
 
ALX-450-006 Revised 07-Apr-08
Ionomycin (free acid)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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ALX-450-006-M001   1 mg 75.00 USD Add To Cart
ALX-450-006-M005   5 mg 290.00 USD Add To Cart
Product Specification
FORMULA: C41H72O9
MW: 709.0
CAS NUMBER: 56092-81-0
SOURCE/HOST: Isolated from Streptomyces conglobatus.
PURITY: ≥90%
APPEARANCE: Pale-yellow oil.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for 1 year when stored at +4°C.
HANDLING: Protect from light. Keep under inert gas.
HAZARD: HARMFUL.

Product Description
Potent and selective calcium ionophore. Ca2+/ionomycin complex forms between pH 7-9.5 which has intense UV absorption. Induces apoptotic neuronal degeneration in embryonic cortical neurons and cell cycle arrest at G1 phase.
Product Specific Literature References
Characterization of ionomycin as a calcium ionophore: C.M. Liu & T.E. Herman; J. Biol. Chem. 253, 5892 (1978) Abstract; Full Text
Structure of ionomycin - a novel diacidic polyether antibiotic having high affinity for calcium ions: B.K. Toeplitz at al.; JACS 101, 3344 (1979)
Demonstration of a calcium requirement for secretory protein processing and export. Differential effects of calcium and dithiothreitol: G. Kuznetsov, et al.; J. Biol. Chem. 267, 3932 (1992) Abstract; Full Text
Potentiation of calcium- and caffeine-induced calcium release by cyclic ADP-ribose: H.C. Lee; J. Biol. Chem. 268, 293 (1993) Abstract; Full Text
Contrasting effect of transforming growth factor type beta 1 (TGF-beta 1) on proliferation and interleukin-2 receptor expression in activated and rapidly cycling immature (CD3-CD4-CD8-) thymocytes: A. Dupuy d'Angeac, et al.; J. Cell. Physiol. 154, 44 (1993) Abstract
Ca2+ ionophore-induced apoptosis on cultured embryonic rat cortical neurons: N. Takei & Y. Endo; Brain Res. 652, 65 (1994) Abstract
Differential activation of a calcium-dependent endonuclease in human B lymphocytes. Role in ionomycin-induced apoptosis: K.M. Aagaard-Tillery & D.F. Jelinek; J. Immunol. 155, 3297 (1995) Abstract
ctivation of stress response by ionomycin in rat hepatoma cells: A. S. Sreedhar & U. K. Srinivas; J. Cell. Biochem. 86, 154 (2002) Abstract
Ionomycin downregulates beta-catenin/Tcf signaling in colon cancer cell line: C.H. Park, et al.; Carcinogenesis 26, 1929 (2005) Abstract
Further Categories Containing This Product:
Antibiotics - Apoptosis Inducers & Inhibitors • Antibiotics for Cell Cycle Research • Cell Cycle Blockers & Inhibitors / Related Products
 
 
ALX-450-007 Revised 20-Aug-08
Ionomycin . calcium salt
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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ALX-450-007-M001   1 mg 80.00 USD Add To Cart
ALX-450-007-M005   5 mg 320.00 USD Add To Cart
Product Specification
FORMULA: C41H70O9 . Ca
MW: 707.0 . 40.1
CAS NUMBER: 56092-82-1
SOURCE/HOST: Isolated from Streptomyces conglobatus.
PURITY: ≥97%
APPEARANCE: White solid.
SOLUBILITY: 10mg/ml soluble in DMSO or 100% ethanol, 5mg/ml soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
For technical information and literature references see Ionomycin (free acid) (Prod. No. ALX-450-006).
Further Categories Containing This Product: