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ALX-350-019

Revised 16-Oct-08

(+)-Brefeldin A
SYNONYMS	BFA Ascotoxin Decumbin
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Antibiotics - Apoptosis Inducers & Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-019-M005		5 mg	80.00 USD
ALX-350-019-M010		10 mg	130.00 USD
ALX-350-019-M025		25 mg	270.00 USD
ALX-350-019-M050		50 mg	420.00 USD

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-350-307

Revised 05-Apr-08

Gonyautoxin 2/3 Epimers
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Neurotoxins

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-307-C010		10 µg	230.00 USD

Product Specification

FORMULA:	C₁₀H₁₇N₇O₈S
MW:	395.4
CAS NUMBER:	60508-89-6 (GTX II); 60537-65-7 (GTX III)
SOURCE/HOST:	Isolated from Alexandrium tamarense.
CONCENTRATION:	~5.08µg/ml (GTX II); ~1.96µg/ml (GTX III)
PURITY:	≥95%
APPEARANCE:	Liquid. Solution in 0.3M acetic acid.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	TOXIC.

Product Description

Neurotoxin. Epimeric mixture of gonyautoxin 2 (GTX II, C-11α-hydroxysaxitoxinsulfate) and gonyautoxin 3 (GTX III, C-11β-hydroxysaxitoxinsulfate). Equally potent and selective Na⁺ channel blockers.

Product Specific Literature References

Letter: Structures of gonyautoxin II and III from the East Coast toxic dinoflagellate Gonyaulax tamarensis: Y. Shimizu, et al.; JACS 98, 5414 (1976) Abstract
Gonyautoxin associated with RNA-containing fraction in the toxic scallop digestive gland: M. Kodama, et al.; J. Biochem. 92, 105 (1982) Abstract
Structure and function of voltage-gated sodium channels: E. Marban, et al.; J. Physiol. 508 (Pt 3), 647 (1998) Abstract; Full Text
Toxicokinetics and toxicodynamics of gonyautoxins after an oral toxin dose in cats: D. Andrinolo, et al.; Toxicon 40, 699 (2002) Abstract
The gonyautoxin 2/3 epimers reduces anal tone when injected in the anal sphincter of healthy adults: R. Garrido, et al.; Biol. Res. 37, 395 (2004) Abstract
Gonyautoxin: new treatment for healing acute and chronic anal fissures: R. Garrido, et al.; Dis. Colon Rectum 48, 335 (2005) Abstract

Further Categories Containing This Product:

Na+ Channels • Marine Natural Products

ALX-440-043

Revised 07-Jun-05

Triamterene
SYNONYMS	6-Phenyl-2,4,7-pteridinetriamine
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Na+ Channels

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-440-043-G005		5 g	25.00 USD

Product Specification

FORMULA:	C₁₂H₁₁N₇
MW:	253.3
CAS NUMBER:	396-01-0
MERCK INDEX:	14: 9599
PURITY:	≥98%
APPEARANCE:	Yellow solid.
SOLUBILITY:	Soluble in formic acid (50 mg/ml; warm); also soluble in DMSO; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C

Product Description

Na⁺ channel blocker. Diuretic.

ALX-550-212

Revised 17-Jan-05

Amiloride . hydrochloride
SYNONYMS	3,5-Diamino-N-(aminoiminomethyl)-6-chloropyrazinecarboxamide . HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Na+ Channels

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-212-G001		1 g	23.00 USD

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-550-232

Revised 13-May-08

Aconitine
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

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-232-M025		25 mg	45.00 USD

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-550-235

Revised 08-Aug-08

Benzamil . hydrochloride
SYNONYMS	Benzylamiloride . HCl N-(Benzylamidino)-3,5-diamino-6-chloropyrazinecarboxamide . HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Na+ Channels

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-235-M005		5 mg	25.00 USD
ALX-550-235-M025		25 mg	95.00 USD

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-550-238

Revised 03-Feb-05

Bumetanide
SYNONYMS	Ro 10-6338 3-(Aminosulfonyl)-5-(butylamino)-4-phenoxybenzoic acid
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Na+ Channels

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-238-M500		500 mg	40.00 USD
ALX-550-238-G001		1 g	60.00 USD

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-550-251

Revised 22-May-07

Lidocaine . hydrochloride
SYNONYMS	2-Diethylamino-N-(2',6'-dimethylphenyl)acetamide . HCl
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Na+ Channels

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-251-G005		5 g	10.00 USD

Product Specification

FORMULA:	C₁₄H₂₂N₂O . HCl
MW:	234.3 . 36.5
CAS NUMBER:	6108-05-0
MERCK INDEX:	14: 5482
RTECS:	AN7700000
PURITY:	≥98%
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+20°C
HAZARD:	HARMFUL.

Product Description

Na⁺ channel blocker.

Product Specific Literature References

Antiarrhythmic drugs: clinical pharmacology and therapeutic uses: J.L. Anderson, et al.; Drugs 15, 271 (1978) Abstract
Selectivity of antiarrhythmic drugs and ionic channels: a historical overview: E. Carmeliet; Ann. N. Y. Acad. Sci. 427, 1 (1984) Abstract

ALX-550-252

Revised 04-Feb-05

Lidocaine N-ethyl bromide (quaternary salt)
SYNONYMS	QX-314 N-(2,6-Dimethylphenylcarbamoylmethyl)triethylammonium bromide
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Na+ Channels

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-252-M010		10 mg	20.00 USD
ALX-550-252-M050		50 mg	80.00 USD

Product Specification

FORMULA:	C₁₆H₂₇BrN₂O
MW:	343.3
CAS NUMBER:	21306-56-9
PURITY:	≥99%
APPEARANCE:	White solid.
SOLUBILITY:	Soluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light.

Product Description

Quaternary derivative of lidocaine (Prod. No. ALX-550-251) that is not membrane permeable. Blocks both fast, Na⁺-dependent action potentials and voltage-dependent, non-inactivating Na⁺ conductance.

Product Specific Literature References

Effects of local anesthetic QX-314 on the membrane properties of hippocampal pyramidal neurons: B.W. Connors & D.A. Prince; J. Pharmacol. Exp. Ther. 220, 476 (1982) Abstract
Interactions of monovalent cations with sodium channels in squid axon. II. Modification of pharmacological inactivation gating: J.Z. Yeh & G.S. Oxford; J. Gen. Physiol. 85, 603 (1985) Abstract

Further Categories Containing This Product:

Neuroactive Agents Other Products

ALX-550-257

Revised 10-Feb-05

Amiloride, 5-(N-Methyl-N-isobutyl)-
SYNONYMS	5-(N-Methyl-N-isobutyl)amiloride MIA
PRODUCT LINE	Signal Transduction
PRODUCT CATEGORY	Na+ Channels

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-550-257-M005		5 mg	25.00 USD

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)