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Ion Channels & Transporters / Related Products
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ALX-550-266 Revised 12-Feb-08
Amiloride, 5-(N-Ethyl-N-isopropyl)-
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SYNONYMS 5-(N-Ethyl-N-isopropyl)amiloride
EIPA
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-266-M005   5 mg 38.00 USD Add To Cart
Product Specification
FORMULA: C11H18ClN7O
MW: 299.8
CAS NUMBER: 1154-25-2
PURITY: ≥99%
APPEARANCE: Off-white to yellow solid.
SOLUBILITY: Soluble in methanol, DMSO or dilute aqueous acid; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Selective inhibitor of the Na+/H+ antiporter.
Product Specific Literature References
Influence of atrial natriuretic factor on 5-(N-ethyl-N- isopropyl)amiloride-sensitive 22Na+ uptake in rabbit aorta: S. Gupta, et al.; J. Pharmacol. Exp. Ther. 248, 991 (1989) Abstract
Regulation of intracellular pH in crypt cells from rabbit distal colon: S.L. Abrahamse, et al.; Am. J. Physiol. 267, G409 (1994) Abstract
Apical membrane Na+/H+ exchange in rat medullary thick ascending limb. pH-dependence and inhibition by hyperosmolality: B.A. Watts III & D.W. Good; J. Biol. Chem. 269, 20250 (1994) Abstract; Full Text
Further Categories Containing This Product:
Imidazoline Binding Site Ligands • Ca2+ Channels (T-type)
 
 
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
Further Categories Containing This Product:
Cytochrome P450 [CYP450] / Related Products • PPAR Agonists • PLA2 Inhibitors • Ca2+ Modulators • COX Inhibitors
 
 
ALX-550-072 Revised 28-Jan-05
Dantrolene . sodium salt
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-072-M010   10 mg 14.00 USD Add To Cart
ALX-550-072-M050   50 mg 32.00 USD Add To Cart
Product Specification
FORMULA: C14H9N4O5Na
MW: 336.2
CAS NUMBER: 14663-23-1
MERCK INDEX: 14: 2816
PURITY: ≥99%
APPEARANCE: Orange solid.
SOLUBILITY: Soluble in DMSO; insoluble in dilute aqueous base or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Inhibitor of Ca2+ release from intracellular stores, probably by binding to the ryanodine receptor. Intracellularly acting muscle relaxant.
Product Specific Literature References
1-[(5-arylfurfurylidene)amino]hydantoins. A new class of muscle relaxants: Snyder, et al.; J. Med. Chem. 10, 807 (1967) Abstract
Dantrolene. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic use in malignant hyperthermia, the neuroleptic malignant syndrome and an update of its use in muscle spasticity: A. Ward, et al.; Drugs 32, 130 (1986) Abstract
Dantrolene sodium diminishes exercise-induced muscle damage in the rat: G.J. Amelink, et al.; Eur. J. Pharmacol. 179, 187 (1990) Abstract
Inhibitory action of dantrolene on Ca-induced Ca2+ release from sarcoplasmic reticulum in guinea pig skeletal muscle: T. Ohta, et al.; Eur. J. Pharmacol. 178, 11 (1990) Abstract
Mobilization of dantrolene-sensitive intracellular calcium pools is involved in the cytotoxicity induced by quisqualate and N-methyl-D-aspartate but not by 2amino3(3hydroxy5methylisoxazol4yl)propionate and kainate in cultured cerebral cortical neurons: A. Frandsen & A. Schousboe; PNAS 89, 2590 (1992) Abstract
Increased intracellular Ca2+: a critical link in the pathophysiology of sepsis?: S.K. Song, et al.; PNAS 90, 3933 (1993) Abstract
Possible mechanism of dantrolene stabilization of cultured neuroblastoma cell plasma membranes: T. Hayashi, et al.; J. Neurochem. 63, 1849 (1994) Abstract
NMDA receptor-dependent excitotoxicity: the role of intracellular Ca2+ release: I. Mody & J.F. McDonald; TIPS 16, 356 (1995), (Review) Abstract
 
 
ALX-550-237 Revised 18-Jan-05
Bepridil . hydrochloride
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SYNONYMS 1-Isobutoxy-2-pyrrolidino-3-(N-benzylanilino)propane . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-237-M010   10 mg 25.00 USD Add To Cart
ALX-550-237-M025   25 mg 55.00 USD Add To Cart
Product Specification
FORMULA: C24H34N2O . HCl
MW: 366.6 . 36.5
CAS NUMBER: 74764-40-2
MERCK INDEX: 14: 1150
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in 100% ethanol; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Store tightly sealed.

Product Description
Non-selective Ca2+ channel blocker. Stimulates the binding of 1,4-dihydropyridine-based drugs to Ca2+ channels. Inhibits Na+/Ca2+ exchange.
Product Specific Literature References
Characterization and photoaffinity labeling of receptor sites for the Ca2+ channel inhibitors d-cis-diltiazem, (+/-)-bepridil, desmethoxyverapamil, and (+)-PN 200-110 in skeletal muscle transverse tubule membranes: J.P. Galizzi, et al.; J. Biol. Chem. 261, 1393 (1986) Abstract; Full Text
Drug action and cellular calcium regulation: R. Janis, et al.; Adv. Drug Res. 16, 309 (1987)
Bepridil as an antisickling agent: membrane internalization and cell rigidity: R.M. Johnson, et al.; Am. J. Hematol. 46, 310 (1994) Abstract
Intracellular Ca2+ mediates the cytotoxicity induced by bepridil and benzamil in human brain tumor cells: Y.S. Lee, et al.; Cancer Lett. 88, 87 (1995) Abstract
 
 
ALX-550-253 Revised 30-Nov-04
Loperamide . hydrochloride
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SYNONYMS 4-(p-Chlorophenyl)-4-hydroxy-N,N-dimethyl-α,α-diphenyl-1-piperidinebutyramide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-253-G001   1 g 15.00 USD Add To Cart
ALX-550-253-G005   5 g 55.00 USD Add To Cart
Product Specification
FORMULA: C29H33ClN2O2 . HCl
MW: 477.1 . 36.5
CAS NUMBER: 34552-83-5
MERCK INDEX: 14: 5571
PURITY: ≥99%
APPEARANCE: White powder.
SOLUBILITY: Soluble in methanol or chloroform.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Non-selective Ca2+ channel blocker. At nanomolar concentrations, binds to opioid μ-receptors. Does not cross the blood brain barrier.
Product Specific Literature References
Loperamide: blockade of calcium channels as a mechanism for antidiarrheal effects: I.J. Reynolds, et al.; J. Pharmacol. Exp. Ther. 231, 628 (1984) Abstract
Further Categories Containing This Product:
Opioid Receptors / Related Products
 
 
ALX-550-264 Revised 13-Nov-02
Dotarizine
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SYNONYMS 1-(Diphenylmethyl)-4-[3-(2-phenyl-1,3-dioxolan-2-yl)]piperazine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-264-M005   5 mg 80.00 USD Add To Cart
ALX-550-264-M025   25 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C29H34N2O2
MW: 442.6
CAS NUMBER: 84625-59-2
MERCK INDEX: 14: 3428
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
Blocks Ca2+ entry through Ca2+ channels.
Product Specific Literature References
Effects of dotarizine on 45Ca2+ movements and contractile responses in vascular smooth muscle: T. Tejerina, et al.; Eur. J. Pharmacol. 239, 75 (1993) Abstract
 
 
ALX-550-270 Revised 22-May-07
Glibenclamide
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SYNONYMS Glyburide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-550-270-G001   1 g 17.00 USD Add To Cart
Product Specification
FORMULA: C23H28ClN3O5S
MW: 494.0
CAS NUMBER: 10238-21-8
MERCK INDEX: 14: 4478
RTECS: YS4725200
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO (25mg/ml) or 100% ethanol (5mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Solutions are stable for up to 3 months when stored at -20°C.
HAZARD: HARMFUL.

Product Description
ATP-dependent K+ channel blocker in the pancreas, which in turn causes intracellular Ca2+ levels to rise and for insulin to be secreted. Antidiabetic. High affinity binding sites have been identified in the cardiovascular system, the CNS, and pancreatic beta cells. Large potency differences are observed between pancreatic tissue and vascular tissue.
Product Specific Literature References
Glipizide: a review of its pharmacological properties and therapeutic use: R.N. Brogden, et al.; Drugs 18, 329 (1979) Abstract
Intracellular ATP directly blocks K+ channels in pancreatic B-cells: D.L. Cook & C.N. Hales; Nature 311, 271 (1984) Abstract
Antidiabetic sulfonylureas control action potential properties in heart cells via high affinity receptors that are linked to ATP-dependent K+ channels: M. Fosset, et al.; J. Biol. Chem. 263, 7933 (1988) Abstract; Full Text
In vitro effects of sulfonylurea on glucose transport and translocation of glucose transporters in adipocytes from streptozocin-induced diabetic rats: D.R. Jacobs, et al.; Diabetes 38, 205 (1989) Abstract
Glyburide blocks the relaxation response to BRL 34915 (cromakalim), minoxidil sulfate and diazoxide in vascular smooth muscle: R.J. Winquist, et al.; J. Pharmacol. Exp. Ther. 248, 149 (1989) Abstract
Potassium channel modulators: scientific applications and therapeutic promise: D.W. Robertson & M.I. Steinberg; J. Med. Chem. 33, 1529 (1990) Abstract
D.R. Gehlert, et al.; J. Pharmacol. Exp. Ther. 257, 901 (1991) Abstract
High affinity [3H]glibenclamide binding sites in rat neuronal and cardiac tissue: localization and developmental characteristics: J.A. Miller, et al.; J. Pharmacol. Exp. Ther. 256, 358 (1991) Abstract
Glyburide and tolbutamide induce desensitization of insulin release in rat pancreatic islets by different mechanisms: A.M. Rabuazzo, et al.; Endocrinology 131, 1815 (1992) Abstract
Further Categories Containing This Product:
Ca2+ Modulators • Antidiabetic Agents / Related Products
 
 
ALX-550-297 Revised 22-Sep-08
SKF-96365 . hydrochloride
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SYNONYMS 1-[β-[3-(4-Methoxyphenyl)propoxy]-4-methoxyphenethyl]-1H-imidazole . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-297-M001   1 mg 37.00 USD Add To Cart
ALX-550-297-M005   5 mg 88.00 USD Add To Cart
Product Specification
FORMULA: C22H26N2O3 . HCl
MW: 366.5 . 36.5
CAS NUMBER: 130495-35-1
PURITY: ≥98% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water (30mg/ml) or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
USE/STABILITY: Stock solutions are stable for up to 3 months at -20°C.

Product Description
Inhibits voltage-gated Ca2+ channels. Inhibits the histamine-induced formation of nitric oxide in human endothelial cells.
Product Specific Literature References
SKF 96365, a novel inhibitor of receptor-mediated calcium entry: J.E. Merritt, et al.; Biochem. J. 271, 515 (1990) Abstract
Inhibition of a receptor-operated calcium channel in pig aortic microsomes by cyclic GMP-dependent protein kinase: L.M. Blayney, et al.; Biochem. J. 273, 803 (1991) Abstract
SKF 96365 inhibits histamine-induced formation of endothelium-derived relaxing factor in human endothelial cells: W.F. Graier, et al.; BBRC 186, 1539 (1992) Abstract
Vectorial Ca2+ flux from the extracellular space to the endoplasmic reticulum via a restricted cytoplasmic compartment regulates inositol 1,4,5-trisphosphate-stimulated Ca2+ release from internal stores in vascular endothelial cells: O.A. Cabello & W.P. Schilling; Biochem. J. 295, 357 (1993) Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION Product is not sterile.
Further Categories Containing This Product:
Nitric Oxide Pathway Other Products
 
 
ALX-550-299 Revised 09-Oct-06
Thioridazine . hydrochloride
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SYNONYMS 10-[2-(1-Methyl-2-piperidinyl)ethyl]-2-(methylthio)-phenothiazine . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-550-299-G001   1 g 20.00 USD Add To Cart
Product Specification
FORMULA: C21H26N2S2 . HCl
MW: 370.6 . 36.5
CAS NUMBER: 130-61-0
MERCK INDEX: 14: 9359
RTECS: SP2275000
PURITY: ≥99% (TLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol, methanol or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Protect from light.
HAZARD: HARMFUL.

Product Description
Ca2+ channel antagonist. Dopamine inhibitor. Antipsychotic.
Product Specific Literature References
Calcium-antagonist drugs. Receptor interactions that clarify therapeutic effects: S.H. Snyder & I.J. Reynolds; New Engl. J. Med. 313, 995 (1985) Abstract
Further Categories Containing This Product:
Dopaminergics & Dopamine Receptors / Related Products
 
 
ALX-550-307 Revised 09-Sep-08
Veratridine
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SYNONYMS 3-Veratroylveracevine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-307-M005   5 mg