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K+ Channel Blockers & Inhibitors
You are here: Product Lines > Signal Transduction > Ion Channels & Transporters / Related Products > K+ Channels > K+ Channel Blockers & Inhibitors
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ALX-380-056 Revised 10-May-07
Verruculogen
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics for Cell Cycle Research
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ALX-380-056-M001   1 mg 60.00 USD Add To Cart
ALX-380-056-M005   5 mg 225.00 USD Add To Cart
Product Specification
FORMULA: C27H33N3O7
MW: 511.2
CAS NUMBER: 12771-72-1
RTECS: JH4920000
SOURCE/HOST: Isolated from Penicillium verruculosum.
PURITY: ≥96%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in ethyl acetate, DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: VERY TOXIC.

Product Description
Neurotoxin that acts as an inhibitor of the M phase of the mammalian cell cycle. Inhibits Ca2+-activated K+ channels. Decreases GABA levels in CNS.
Product Specific Literature References
Tremorgenic indole alkaloids potently inhibit smooth muscle high- conductance calcium-activated potassium channels: H.H. Knaus, et al.; Biochemistry 33, 5819 (1994) Abstract
Novel mammalian cell cycle inhibitors, tryprostatins A, B and other diketopiperazines produced by Aspergillus fumigatus. II. Physico- chemical properties and structures: C.B. Cui, et al.; J. Antibiot. (Tokyo) 49, 534 (1996) Abstract
Verruculogen production in airborne and clinical isolates of Aspergillus fumigatus Fres.: I. Kosalec, et al.; Acta Pharm. 55, 357 (2005) Abstract
Further Categories Containing This Product:
Alkaloids • Cell Cycle Blockers & Inhibitors / Related Products • K+ Channel Blockers & Inhibitors • Neurotoxins
 
 
ALX-400-012 Revised 29-Jan-05
Tetraethylammonium chloride
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SYNONYMS TEA chloride
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-400-012-G005   5 g 18.00 USD Add To Cart
Product Specification
FORMULA: C8H20ClN
MW: 165.7
CAS NUMBER: 56-34-8
MERCK INDEX: 14: 9200
PURITY: ≥98%
APPEARANCE: White to light yellow solid.
SOLUBILITY: Soluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Hygroscopic.
HAZARD: IRRITANT.

Product Description
K+ channel blocker and antagonist of nicotinic cholinergic receptor. Ganglionic blocking agent.
Product Specific Literature References
Consequences of axonal transport blockade by batrachotoxin on mammalian neuromuscular junction. II. Late pre- and postsynaptic changes: S.S. Deshpande, et al.; Brain Res. 225, 115 (1981) Abstract
Tetraethylammonium contains an impurity which alkalizes cytoplasm and reduce calcium buffering in neurons: R.S. Zucker; Brain Res. 208, 473 (1981) Abstract
Release of TEA blockade of maxi-K+ channels by isoproterenol: S.W. Fan, et al.; BBRC 201, 24 (1994) Abstract
 
 
ALX-430-042 Revised 24-Sep-02
Dequaliniumchloride
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PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-430-042-G001   1 g 25.00 USD Add To Cart
Product Specification
FORMULA: C30H40Cl2N4
MW: 527.6
CAS NUMBER: 522-51-0
MERCK INDEX: 14: 2913
PURITY: ≥95%
APPEARANCE: Off-white powder.
SOLUBILITY: Slightly soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: IRRITANT.

Product Description
Potent and selective non-peptide blocker of the apamin-sensitive small conductance Ca2+-activated K+ channel.
Product Specific Literature References
Dequalinium, a selective blocker of the slow afterhyperpolarization in rat sympathetic neurones in culture: P.M. Dunn; Eur. J. Pharmacol. 252, 189 (1994) Abstract
 
 
ALX-430-111 Revised 31-Mar-08
E-4031 . dihydrochloride
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SYNONYMS 4’-[[1-[2-(6-methyl-2-pyridyl)ethyl]-4-piperidinyl]carbonyl]-methanesulfonanilide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-430-111-M005   5 mg 120.00 USD Add To Cart
Product Specification
FORMULA: C21H27N3O3S . 2HCl
MW: 401.5 . 73.0
CAS NUMBER: 113559-13-0
PURITY: ≥98%
APPEARANCE: White to off-white crystalline powder.
SOLUBILITY: Soluble in water.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: +4°C
HANDLING: Hygroscopic.

Product Description
K+ channel blocker. Lead compound to investigate class III antiarrhythmic drugs. Specific blocker of delayed rectifier current (I(kr)). Blocks the human ether-a-go-go-related gene (HERG) at all pulse frequencies (frequency-independent block) without significant recovery at rest.
Product Specific Literature References
Effects of antiarrhythmic agents classified as class III group on ischaemia-induced myocardial damage in canine hearts: T. Sano, et al.; Br. J. Pharmacol. 99, 577 (1990) Abstract; Full Text
Differential class III and glibenclamide effects on action potential duration in guinea-pig papillary muscle during normoxia and hypoxia/ischaemia: I. MacKenzie, et al.; Br. J. Pharmacol. 110, 531 (1993) Abstract; Full Text
Effects of class III antiarrhythmic drugs on the Na(+)-activated K+ channels in guinea-pig ventricular cells: K. Mori, et al.; Br. J. Pharmacol. 119, 133 (1996) Abstract
Inhibition of potassium currents by the antiarrhythmic drug E4031 in rat taste receptor cells: X.D Sun & M.S. Herness; Neurosci. Lett. 204, 149 (1996) Abstract
Modulation of HERG affinity for E-4031 by [K+]o and C-type inactivation: S. Wang, et al.; FEBS Lett. 417, 43 (1997) Abstract
Effects of divalent cations on the E-4031-sensitive repolarization current, I(Kr), in rabbit ventricular myocytes: T. Paquette, et al.; Biophys. J. 74, 1278 (1998) Abstract; Full Text
E-4031 enhanced Ca2+ transient and ventricular myocytes contraction via reverse mode Na+/Ca2+ exchange in normal and hypertrophic rats: X.L Cui, et al.; Acta Pharmacol. Sin. 23, 797 (2002) Abstract
Functional up-regulation of HERG K+ channels in neoplastic hematopoietic cells: G.A. Smith, et al.; J. Biol. Chem. 277, 18528 (2002) Abstract; Full Text
Expression and function of KCNH2 (HERG) in the human jejunum: A.M. Farrelly; Am. J. Physiol. Gastrointest. Liver Physiol. 284, G883 (2003) Abstract; Full Text
Expression and role of the ether-à-go-go-related (MERG1A) potassium-channel protein during preimplantation mouse development: N.J. Winston, et al.; Biol. Reprod. 70, 1070 (2004) Abstract; Full Text
A rapidly activating delayed rectifier K+ current regulates pacemaker activity in adult mouse sinoatrial node cells: R.B. Clark, et al.; Am. J. Physiol. Heart Circ. Physiol. 286, H1757 (2004) Abstract; Full Text
Single-channel recordings of a rapid delayed rectifier current in adult mouse ventricular myocytes: basic properties and effects of divalent cations: G.X. Liu; J. Physiol. 556, 401 (2004) Abstract; Full Text
Contribution of IKr to rate-dependent action potential dynamics in canine endocardium: F. Hua & R.F. Gilmour Jr.; Circ. Res. 94, 810 (2004) Abstract; Full Text
Postnatal development of E-4031-sensitive potassium current in rat carotid chemoreceptor cells: I. Kim, et al.; J. Appl. Physiol. 98, 1469 (2005) Abstract; Full Text
Molecular determinants of HERG channel block: K. Kamiya, et al.; Mol. Pharmacol. 69, 1709 (2006) Abstract; Full Text
State dependent dissociation of HERG channel inhibitors: D. Stork, et al.; Br. J. Pharmacol. 151, 1368 (2007) Abstract
Role of reverse mode Na+/Ca2+ exchanger in the cardioprotection of metabolic inhibition preconditioning in rat ventricular myocytes: S.Z. Liu, et al.; Eur. J. Phamacol. 561, 14 (2007) Abstract
Pharmacological and biophysical isolation of K+ currents encoded by ether-à-go-go-related genes in murine hepatic portal vein smooth muscle cells: S.Y. Yeung & I.A. Greenwood; Am. J. Physiol. Cell Physiol. 292, C468 (2007) Abstract; Full Text
Characterization of the effects of Ryanodine, TTX, E-4031 and 4-AP on the sinoatrial and atrioventricular nodes: M.R. Nikmaram, et al.; Prog. Biophys. Mol. Biol. 96, 452 (2008) Abstract
 
 
ALX-550-040 Revised 06-Feb-07
(-)-Bicuculline methobromide
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PRODUCT LINE Neurobiology
PRODUCT CATEGORY GABA-ergics & GABA Receptors / Related Products
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ALX-550-040-M010   10 mg 20.00 USD Add To Cart
ALX-550-040-M050   50 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C21H20BrNO6
MW: 462.3
CAS NUMBER: 73604-30-5
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water, 100% ethanol, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
GABAA receptor antagonist. Blocks Ca2+-activated K+ channels.
Product Specific Literature References
3H-baclofen and 3H-GABA bind to bicuculline-insensitive GABA B sites in rat brain: D.R. Hill & N.G. Bowery; Nature 290, 149 (1981) Abstract
Further Categories Containing This Product:
K+ Channel Blockers & Inhibitors
 
 
ALX-550-141 Revised 07-Jan-09
4-Aminopyridine
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SYNONYMS Fampridine
4-Pyridylamine
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-550-141-G005   5 g 20.00 USD Add To Cart
Product Specification
FORMULA: C5H6N2
MW: 94.1
CAS NUMBER: 504-24-5
MERCK INDEX: 14: 3933
RTECS: US1750000
PURITY: ≥98% (TLC)
APPEARANCE: Off-white to tan solid.
SOLUBILITY: Soluble in water (50mg/ml) or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.
HAZARD: VERY TOXIC.
IDENTITY: Identity determined by IR.

Product Description
Induces depolarization of GABA neurons. Non-selective K+ channel blocker. Reverses saxitoxin- and tetrodotoxin-induced cardiorespiratory depression. Increases stimulation-induced release of acetylcholine.
Product Specific Literature References
Effects of 4-aminopyridine on normal and demyelinated mammalian nerve fibres: R.M. Sherratt, et al.; Nature 283, 570 (1980) Abstract
The origin, structure, and pharmacological activity of botulinum toxin: L.L. Simpson; Pharmacol. Rev. 33, 155 (1981) Abstract
Further Categories Containing This Product:
GABA-ergics & GABA Receptors / Related Products
 
 
ALX-550-216 Revised 06-Jul-06
Tolazamide
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SYNONYMS U-17835
N-[[(Hexahydro-1H-azepinyl)amino]carbonyl]-4-methylbenzenesulfonamide
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-550-216-G001   1 g 10.00 USD Add To Cart
ALX-550-216-G005   5 g 35.00 USD Add To Cart
Product Specification
FORMULA: C14H21N3O3S
MW: 311.4
CAS NUMBER: 1156-19-0
MERCK INDEX: 14: 9505
RTECS: YT4400000
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO or dilute aqueous base; insoluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HAZARD: HARMFUL.

Product Description
Selectively blocks ATP-sensitive K+ channels.
 
 
ALX-550-222 Revised 18-Jul-07
SKF-525A . HCl
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SYNONYMS Proadifen
α-Phenyl-α-propylbenzeneacetic acid 2-(diethylamino)ethyl ester
N,N-Diethylaminoethyl 2,2-diphenylvalerate
PRODUCT LINE Nitric Oxide Pathway
PRODUCT CATEGORY NOS Inhibitors (NOS Induction & Enzyme Activity)
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ALX-550-222-M100   100 mg 50.00 USD Add To Cart
ALX-550-222-M250   250 mg 80.00 USD Add To Cart
Product Specification
FORMULA: C23H31NO2 . HCl
MW: 353.5 . 36.5
CAS NUMBER: 62-68-0
RTECS: YV7175000
PURITY: ≥98%
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water or 100% ethanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic.
HAZARD: HARMFUL.

Product Description
Cell permeable inhibitor of neuronal nitric oxide synthase (nNOS; NOS I) (IC50=90µM). Inhibitor of cytochrome P450 system. Calcium antagonist. Blocks glibenclamide-sensitive K+ channels (IC50=4.4mM). Inhibits platelet thromboxane synthesis and stimulates endothelial cell prostacyclin production. Potentiates the effects of many drugs in vivo.
Product Specific Literature References
Effects of 2-diethylaminoethyl 2,2-diphenylpentanoate (SKF 525A) on insecticidal potency: P.S. Hewlett, et al.; Nature 192, 1273 (1961) Abstract
The effects of beta-diethylaminoethyl-diphenylpropylacetate (SKE 525-A) on biological membranes. I. SKF 525-A-induced stabilization of human erythrocytes: I.P. Lee, et al.; Biochem. Pharmacol. 17, 1671 (1968) Abstract
Heterogeneity of cytochrome P-450 in rat liver microsomes: selective interaction of metyrapone and SKF 525-A with different fractions of microsomal cytochrome P-450: H. Grasdalen, et al.; FEBS Lett. 60, 294 (1975) Abstract
Inhibition of mitochondrial oxidative metabolism by SKF-525A in intact cells and isolated mitochondria: T. Galeotti, et al.; Biochem. Pharmacol. 32, 3285 (1983) Abstract
Prostacyclin-stimulating drugs: new prospects: J.M. Boeynaems, et al.; Prostaglandins 32, 145 (1986) Abstract
Defining the active site of cytochrome P-450: the crystal and molecular structure of an inhibitor, SKF-525A: M. Rossi, et al.; Carcinogenesis 8, 881 (1987) Abstract
Stimulation of vascular prostacyclin by SKF 525-A (proadifen) and related compounds: J.M. Boeynaems, et al.; Biochem. Pharmacol. 36, 1637 (1987) Abstract
Effect of SKF 525A on the release of nitric oxide and prostacyclin from endothelial cells: D.D. Rees, et al.; Eur. J. Pharmacol. 150, 149 (1988) Abstract
Subcellular localization and characterization of neuronal nitric oxide synthase: M. Hecker, et al.; J. Neurochem. 62, 1524 (1994) Abstract
Inhibition by SKF 525A and quinacrine of endogenous glibenclamide-sensitive K+ channels in follicle-enclosed Xenopus oocytes: H. Sakuta & I. Yoneda; Eur. J. Pharmacol. 252, 117 (1994) Abstract
Further Categories Containing This Product:
K+ Channel Blockers & Inhibitors • Cytochrome P450 [CYP450] / Related Products
 
 
ALX-550-242 Revised 23-Jul-04
Clofilium . tosylate
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SYNONYMS 4-Chloro-N,N-diethyl-N-heptylbenzenebutanaminium . tosylate
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-550-242-M025   25 mg 40.00 USD Add To Cart
ALX-550-242-M100   100 mg 120.00 USD Add To Cart
ALX-550-242-M250   250 mg 240.00 USD Add To Cart
Product Specification
FORMULA: C21H37ClN . C7H7O3S
MW: 339.0 . 171.2
CAS NUMBER: 92953-10-1
PURITY: ≥97%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water, methanol or DMSO.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C

Product Description
K+ channel blocker. Antiarrhytmic. Cardiac depressant.
Product Specific Literature References
The differential response of normal and ischaemic Purkinje fibres to clofilium, d-sotalol and bretylium: W.B. Gough & N. el-Sherif; Cardiovasc. Res. 23, 554 (1989) Abstract
Block of heart potassium channels by clofilium and its tertiary analogs: relationship between drug structure and type of channel blocked: J.P. Arena & R.S. Kass; Mol. Pharmacol. 34, 60 (1988) Abstract
 
 
ALX-550-263 Revised 03-Feb-05
R-(+)-DIOA
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SYNONYMS R-(+)-Butylindazone
(Dihydroindenyl)oxy alkanoic acid
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY K+ Channel Blockers & Inhibitors
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ALX-550-263-M005   5 mg 40.00 USD Add To Cart
ALX-550-263-M025   25 mg 160.00 USD Add To Cart
Product Specification
FORMULA: C20H24Cl2O4
MW: 399.3
CAS NUMBER: 81166-47-4
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in 100% ethanol or dilute aqueous base; insoluble in water or dilute aqueous acid.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C