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Na+ Channels
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ALX-550-232 Revised 13-May-08
Aconitine
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SYNONYMS (1α,3α,6α,14α,15α,16β)-20-Ethyl-1,6,16-trimethoxy-4-(methoxymethyl)aconitane-3,8,13,14,15-pentol 8-acetate 14-benzoate
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Neurotoxins
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ALX-550-232-M025   25 mg 45.00 USD Add To Cart
Product Specification
FORMULA: C34H47NO11
MW: 645.7
CAS NUMBER: 302-27-2
MERCK INDEX: 14: 118
RTECS: AR5960000
SOURCE/HOST: Isolated from Aconitum karacolium.
PURITY: ≥98%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in 100% ethanol (35mg/ml); almost insoluble in water (0.3mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: VERY TOXIC.

Product Description
A lipid-soluble neurotoxin that acts as a sodium channel modulator. Blocks tetrodotoxin-sensitive Na+ channels. Potent neurotoxin.
Product Specific Literature References
Non-quantal acetylcholine release at mouse neuromuscular junction: effects of elevated quantal release and aconitine: S.P. Yu & W. Van der Kloot; Neurosci. Lett. 117, 111 (1990) Abstract
Synthesis and activity of a potent N-methyl-D-aspartic acid agonist, trans-1-aminocyclobutane-1,3-dicarboxylic acid, and related phosphonic and carboxylic acids: M. Muroi, et al.; Neuropharmacology 29, 567 (1990) Abstract
Further Categories Containing This Product:
Na+ Channels • Alkaloids
 
 
ALX-550-212 Revised 17-Jan-05
Amiloride . hydrochloride
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SYNONYMS 3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-212-G001   1 g 23.00 USD Add To Cart
Product Specification
FORMULA: C6H8ClN7O . HCl
MW: 229.6 . 36.5
CAS NUMBER: 2016-88-8
MERCK INDEX: 14: 406
PURITY: ≥98%
APPEARANCE: Light yellow solid.
SOLUBILITY: Soluble in DMSO or water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: TOXIC.

Product Description
Epithelial Na+ channel inhibitor [1]. Selective T-type Ca2+ channel blocker [2].
Product Specific Literature References
[1] Amiloride and its analogs as tools in the study of ion transport: T.R. Kleyman and E.J. Kragoe Jr.; J. Membr. Biol. 105, 1 (1988) Abstract
[2] Amiloride selectively blocks the low threshold (T) calcium channel: C.-M. Tang, et al.; Science 240, 213 (1988) Abstract
Further Categories Containing This Product:
Ca2+ Channels (T-type) • Imidazoline Binding Site Ligands
 
 
ALX-550-261 Revised 16-Apr-05
Amiloride, 5-(N,N-Dimethyl)-, . hydrochloride
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SYNONYMS 5-(N,N-Dimethyl)amiloride . HCl
DMA . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-261-M005   5 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C8H12ClN7O . HCl
MW: 257.7 . 36.5
CAS NUMBER: 1214-79-5 (free base)
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in methanol (10mg/ml) or water (6mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Na+/H+ antiporter inhibitor (IC50=6.9 µM) with increased selectivity and potency relative to amiloride (Prod. No. ALX-550-212).
Product Specific Literature References
Involvement of sodium in the protective effect of 5-(N,N-dimethyl)- amiloride on ischemia-reperfusion injury in isolated rat ventricular wall: H. Meng & G.N. Pierce; J. Pharmacol. Exp. Ther. 256, 1094 (1991) Abstract
Amiloride and its analogs as tools in the study of ion transport: T.R. Kleyman & E.J. Cragoe Jr.; J. Membr. Biol. 105, 1 (1988) Abstract
Effect of 5-(N,N-Dimethyl)-amiloride, a specific inhibitor of Na(+)/H(+) exchanger, on the palmitoyl-L-carnitine-induced mechanical and metabolic derangements in the isolated perfused rat heart: J. Arakawa & A. Hara; Pharmacology 59, 239 (1999) Abstract
Hypericin-induced phototoxicity of human leukemic cell line HL-60 is potentiated by omeprazole, an inhibitor of H+K+-ATPase and 5'-(N,N-dimethyl)-amiloride, an inhibitor of Na+/H+ exchanger: L. Mirossay, et al.; Physiol. Res. 48, 135 (1999) Abstract
Further Categories Containing This Product:
Imidazoline Binding Site Ligands • Ca2+ Channels (T-type)
 
 
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-550-257 Revised 10-Feb-05
Amiloride, 5-(N-Methyl-N-isobutyl)-
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SYNONYMS 5-(N-Methyl-N-isobutyl)amiloride
MIA
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-257-M005   5 mg 25.00 USD Add To Cart
Product Specification
FORMULA: C11H18ClN7O
MW: 299.8
CAS NUMBER: 96861-65-3
PURITY: ≥98%
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in dilute aqueous acid or DMSO; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Potent inhibitor of the Na+/H+ antiporter. Possible antitumor agent.
Product Specific Literature References
Interactions of chloride and amiloride with the renal Na+/H/ antiporter: D.G. Warnock, et al.; J. Biol. Chem. 263, 7216 (1988) Abstract; Full Text
Methyl isobutyl amiloride: a new probe to assess the number of Na-H antiporters: Z. Talor, et al.; Life Sci. 45, 517 (1989) Abstract
Therapeutic potential of analogues of amiloride: inhibition of the regulation of intracellular pH as a possible mechanism of tumour selective therapy: R.P. Maidorn, et al.; Br. J. Cancer. 67, 297 (1993) Abstract
Study of fibroblast spreading: pH dependence, involvement of the Na+/H(+)-antiporter and PKC: I.Y. Novikova, et al.; Biochim. Biophys. Acta 1178, 267 (1993) Abstract
Methyl isobutyl amiloride alters regional brain reperfusion after resuscitation from cardiac arrest in rats: K.L. Lauro, et al.; Brain Res. 831, 64 (1999) Abstract
Role of Na(+)/H(+) exchanger during ischemia and preconditioning in the isolated rat heart: X.H. Xiao & D.G. Allen; Circ. Res. 85, 723 (1999) Abstract
Further Categories Containing This Product:
Imidazoline Binding Site Ligands • Ca2+ Channels (T-type) • Antitumor Reagents Other Products
 
 
ALX-550-235 Revised 08-Aug-08
Benzamil . hydrochloride
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SYNONYMS Benzylamiloride . HCl
N-(Benzylamidino)-3,5-diamino-6-chloropyrazinecarboxamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-235-M005   5 mg 25.00 USD Add To Cart
ALX-550-235-M025   25 mg 95.00 USD Add To Cart
Product Specification
FORMULA: C13H14ClN7O . HCl
MW: 319.8 . 36.5
CAS NUMBER: 2898-76-2
PURITY: ≥98% (TLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in water or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING: Protect from light.
HAZARD: IRRITANT.

Product Description
Derivative of amiloride (Prod. No. ALX-550-212). Potent Na+ channel blocker.
Product Specific Literature References
Amiloride and its analogs as tools in the study of ion transport: T.R. Kleyman & E.J. Cragoe, Jr; J. Membr. Biol. 105, 1 (1988) Abstract
Structure-activity relations of amiloride and its analogues in blocking the mechanosensitive channel in Xenopus oocytes: J.W. Lane, et al.; Br. J. Pharmacol. 106, 283 (1992) Abstract
Modulation of cardiac performance by amiloride and several selected derivatives of amiloride: G.N. Pierce, et al.; J. Pharmacol. Exp. Ther. 265, 1280 (1993) Abstract
 
 
ALX-350-019 Revised 16-Oct-08
(+)-Brefeldin A
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SYNONYMS BFA
Ascotoxin
Decumbin
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Apoptosis Inducers & Inhibitors
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ALX-350-019-M005   5 mg 80.00 USD Add To Cart
ALX-350-019-M010   10 mg 130.00 USD Add To Cart
ALX-350-019-M025   25 mg 270.00 USD Add To Cart
ALX-350-019-M050   50 mg 420.00 USD Add To Cart
Product Specification
FORMULA: C16H24O4
MW: 280.4
CAS NUMBER: 20350-15-6
MERCK INDEX: 14: 1369
SOURCE/HOST: Isolated from Eupenicillium brefeldianum.
PURITY: ≥97% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, methanol, acetone or ethyl acetate.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.

Product Description
Inhibitor of intracellular protein transport and protein secretion, interfering with trafficking in the trans-Golgi network, leading to the accumulation of cycling proteins in ERGIC clusters. Blocks ADP-ribosylation factor (Arf) in an inactive GDP-bound conformation and thereby prevents binding of COPI coats to ERGIC and Golgi membranes. Upon brefeldin A treatment the Golgi rapidly tubulates and fuses with the ER by an energy-, temperature-, and microtubule-dependent process. In contrast, the drug has little effect on the ERGIC, which keeps its identity, although the ERGIC clusters become larger and more uniformly distributed in the cytoplasm of the cells. Inhibits intracellular collagen degradation. Also inhibits apical Na+ channels in epithelia. Induces apoptosis.
Product Specific Literature References
Decumbin, a new compound from a species of Penicillium: V.L. Singleton, et al.; Nature 181, 1072 (1958)
Über die Isolierung neuer Stoffwechselprodukte aus Penicillium brefeldianum Dodge.: E. Harri, et al.; Helv. Chim. Acta 46, 1235 (1963)
Novel blockade by brefeldin A of intracellular transport of secretory proteins in cultured rat hepatocytes: Y. Misumi, et al.; J. Biol. Chem. 261, 11398 (1986) Abstract; Full Text
Brefeldin A causes disassembly of the Golgi complex and accumulation of secretory proteins in the endoplasmic reticulum: T. Fujiwara, et al.; J. Biol. Chem. 263, 18545 (1988) Abstract; Full Text
Brefeldin A, thapsigargin, and AIF4- stimulate the accumulation of GRP78 mRNA in a cycloheximide dependent manner, whilst induction by hypoxia is independent of protein synthesis: B.D. Price, et al.; J. Cell. Physiol. 152, 545 (1992) Abstract
Brefeldin A and the endocytic pathway. Possible implications for membrane traffic and sorting: W. Hunziker, et al.; FEBS Lett. 307, 93 (1992), (Review) Abstract
Brefeldin A inhibits degradation as well as production and secretion of collagen in human lung fibroblasts: C.R. Ripley, et al.; J. Biol. Chem. 268, 3677 (1993) Abstract
Brefeldin A is a potent inducer of apoptosis in human cancer cells independently of p53: R.G. Shao, et al.; Exp. Cell Res. 227, 190 (1996) Abstract
Brefeldin A inhibition of apical Na+ channels in epithelia: R.S. Fisher, et al.; Am. J. Physiol. 270, C138 (1996) Abstract
Brefeldin A: deciphering an enigmatic inhibitor of secretion: A. Nebenfuhr, et al.; Plant Physiol. 130, 1102 (2002), Review Abstract
NKT cells provide help for dendritic cell-dependent priming of MHC class I-restricted CD8+ T cells in vivo: D. Stober, et al.; J. Immunol. 170, 2540 (2003) Abstract; Full Text
Interaction of BIG2, a brefeldin A-inhibited guanine nucleotide-exchange protein, with exocyst protein Exo70: K.F. Xu, et al.; PNAS 102, 2784 (2005) Abstract
Further Categories Containing This Product:
ADP Ribosylation Factor [ARF] / Related Products • Golgi Apparatus • Collagen / Related Products • Na+ Channels • Antitumor Antibiotics • Antibiotics - Antiviral / Anti-HIV • Antibiotics - Antifungal • Autophagy Other Products • Antitumor Agents (Apoptosis Inducers)
 
 
ALX-550-238 Revised 03-Feb-05
Bumetanide
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SYNONYMS Ro 10-6338
3-(Aminosulfonyl)-5-(butylamino)-4-phenoxybenzoic acid
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Na+ Channels
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ALX-550-238-M500   500 mg 40.00 USD Add To Cart
ALX-550-238-G001   1 g 60.00 USD Add To Cart
Product Specification
FORMULA: C17H20N2O5S
MW: 364.4
CAS NUMBER: 28395-03-1
MERCK INDEX: 14: 1484
PURITY: ≥99%
APPEARANCE: White solid.
SOLUBILITY: Soluble in ethanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: TOXIC.

Product Description
Specific inhibitor of Na+/K+/2Cl- cotransport and is used clinically as a diuretic. Shows high affinity and specific binding to membranes of many cell types.
Product Specific Literature References
Characteristics and functions of Na-K-Cl cotransport in epithelial tissues: S.M. O'Grady, et al.; Am. J. Physiol. 253, C177 (1987) Abstract
Effect of bradykinin on Na-K-2Cl cotransport and bumetanide binding in aortic endothelial cells: J.D. Klein & W.C. O'Neill; J. Biol. Chem. 265, 22238 (1990) Abstract; Full Text
The regulation of Na/K/2Cl cotransport and bumetanide binding in avian erythrocytes by protein phosphorylation and dephosphorylation. Effects of kinase inhibitors and okadaic acid: E.B. Pewitt, et al.; J. Biol. Chem. 265, 20747 (1990) Abstract; Full Text
Pharmacokinetics and pharmacodynamics of the diuretic bumetanide in the elderly: R. Oberbauer, et al.; Clin. Pharmacol. Ther. 57, 42 (1995) Abstract
 
 
ALX-630-054 Revised 14-Oct-08
μ-Conotoxin GIIIB
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Neurotoxins
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ALX-630-054-C500   500 µg 790.00 USD Add To Cart
Product Specification
SEQUENCE: H-Arg-Asp-Cys-Cys-Thr-Hyp-Hyp-Arg-Lys-Cys-Lys-Asp-Arg-Arg-Cys-Lys-Hyp-Met-Lys-Cys-Cys-Ala-NH2
(Disulfide bonds between Cys3-Cys15, Cys4-Cys20and Cys10-Cys21)
FORMULA: C101H175N39O30S7
MW: 2640.2
SOURCE/HOST: Synthetic. Originally isolated from Conus geographus.
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: VERY TOXIC.
Product Description
Neurotoxin. Specific blocker of the skeletal voltage-gated Na+ channels. Not for sale in U.S.A.
Product Specific Literature References
Conus geographus toxins that discriminate between neuronal and muscle sodium channels: L.J. Cruz, et al.; J. Biol. Chem. 260, 9280 (1985) Abstract; Full Text
Use of geographutoxin II (mu-conotoxin) for the study of neuromuscular transmission in mouse: S.J. Hong & C.C. Chang; Br. J. Pharmacol. 97, 934 (1989) Abstract
Noncontractile acetylcholine receptor-operated Ca++ mobilization: suppression of activation by open channel blockers and acceleration of desensitization by closed channel blockers in mouse diaphragm muscle: M. Kimura, et al.; J. Pharmacol. Exp. Ther. 256, 18 (1991) Abstract
Conotoxins: B.M. Olivera, et al.; J. Biol. Chem. 266, 22067 (1991), (Minireview) Abstract; Full Text
Presynaptic calcium signals and transmitter release are modulated by calcium-activated potassium channels: R. Robitaille & M.P. Charlton; J. Neurosci. 12, 297 (1992) Abstract
Solution synthesis of mu-conotoxin GIIIB: optimization of the oxidative folding reaction: S. Kubo, et al.; Pept. Res. 6, 66 (1993) Abstract
Using the deadly mu-conotoxins as probes of voltage-gated sodium channels: R. A. Li & G. F. Tomaselli; Toxicon 44, 117 (2004), (Review) Abstract
Further Categories Containing This Product:
Peptides • Na+ Channels • Marine Natural Products
 
 
ALX-630-047 Revised 14-Oct-08
μ-Conotoxin GS
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Neurotoxins
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-630-047-C500   500 µg 790.00 USD