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Signal Transduction
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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-550-013 Revised 07-May-03
1-Aminocyclobutane-cis-1,3-dicarboxylic acid
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SYNONYMS cis-ACBD
cis-2,4-Methanoglutamic acid
PRODUCT LINE Neurobiology
PRODUCT CATEGORY NMDA Receptors / Related Products
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ALX-550-013-M005   5 mg 65.00 USD Add To Cart
Product Specification
FORMULA: C6H9NO4
MW: 159.1
CAS NUMBER: 117488-23-0
APPEARANCE: White solid.
SOLUBILITY: Soluble in dilute aqueous base.
HANDLING: Protect from light.

Product Description
Very potent and selective NMDA receptor agonist.
Product Specific Literature References
Cis-2,4-methanoglutamate is a potent and selective N-methyl-D-aspartate receptor agonist: T.H. Lanthorn, et al.; Eur. J. Pharmacol. 182, 397 (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: R.D. Allan, et al.; J. Med. Chem. 33, 2905 (1990) Abstract
Inhibition of high affinity L-glutamic acid uptake into rat cortical synaptosomes by the conformationally restricted analogue of glutamic acid, cis-1-aminocyclobutane-1,3-dicarboxylic acid: E.J. Fletcher, et al.; Neurosci. Lett. 121, 133 (1991) Abstract
 
 
ALX-550-073 Revised 16-Dec-04
1-Aminocyclobutane-trans-1,3-dicarboxylic acid
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SYNONYMS trans-ACBD
trans-2,4-Methanoglutamic acid
PRODUCT LINE Neurobiology
PRODUCT CATEGORY NMDA Receptors / Related Products
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ALX-550-073-M005   5 mg 90.00 USD Add To Cart
Product Specification
FORMULA: C6H9NO4
MW: 159.1
CAS NUMBER: 73550-55-7
PURITY: ≥97%
APPEARANCE: White solid.
SOLUBILITY: Soluble in dilute aqueous base.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
Potent and selective inhibitor of glutamate uptake.
Product Specific Literature References
Cis-2,4-methanoglutamate is a potent and selective N-methyl-D-aspartate receptor agonist: T.H. Lanthorn, et al.; Eur. J. Pharmacol. 182, 397 (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: R.D. Allan, et al.; J. Med. Chem. 33, 2905 (1990) Abstract
Inhibition of high affinity L-glutamic acid uptake into rat cortical synaptosomes by the conformationally restricted analogue of glutamic acid, cis-1-aminocyclobutane-1,3-dicarboxylic acid: E.J. Fletcher, et al.; Neurosci. Lett. 121, 133 (1991) Abstract
 
 
ALX-550-014 Revised 29-Nov-04
1-Aminocyclopentanecarboxylic acid
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SYNONYMS ACPC
Cycloleucine
PRODUCT LINE Neurobiology
PRODUCT CATEGORY NMDA Receptors / Related Products
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ALX-550-014-M010   10 mg 17.00 USD Add To Cart
Product Specification
FORMULA: C6H11NO2
MW: 129.2
CAS NUMBER: 52-52-8
MERCK INDEX: 14: 2734
PURITY: ≥98%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light.

Product Description
NMDA receptor antagonist acting at the glycine site.
Product Specific Literature References
1-Aminocyclobutane-1-carboxylate (ACBC): a specific antagonist of the N-methyl-D-aspartate receptor coupled glycine receptor: W.F. Hood, et al.; Eur. J. Pharmacol. 161, 281 (1989) Abstract
 
 
ALX-550-211 Revised 29-Nov-04
1-Aminocyclopropanecarboxylic acid
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SYNONYMS ACPC
PRODUCT LINE Neurobiology
PRODUCT CATEGORY NMDA Receptors / Related Products
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ALX-550-211-M050   50 mg 40.00 USD Add To Cart
Product Specification
FORMULA: C4H7NO2
MW: 101.1
CAS NUMBER: 22059-21-8
PURITY: ≥97%
APPEARANCE: White solid.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +20°C
HANDLING: Hygroscopic.

Product Description
NMDA receptor partial agonist acting at the glycine site.
Product Specific Literature References
1-Aminocyclopropane-1-carboxylic acid (ACC) mimics the effects of glycine on the NMDA receptor ion channel: V. Nadler, et al.; Eur. J. Pharmacol. 157, 115 (1988) Abstract
[3H]1-aminocyclopropanecarboxylic acid, a novel probe for strychnine- insensitive glycine receptors: P. Popik, et al.; Eur. J. Pharmacol. 291, 221 (1995) Abstract
Effect of 1-aminocyclopropanecarboxylic acid on N-methyl-D-aspartate- stimulated [3H]-noradrenaline release in rat hippocampal synaptosomes: M.V. Clos, et al.; Br. J. Pharmacol. 118, 901 (1996) Abstract
 
 
ALX-400-045 Revised 31-Aug-07
2-Aminoethoxydiphenyl borate
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SYNONYMS 2-APB
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
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ALX-400-045-M100   100 mg 30.00 USD Add To Cart
Product Specification
FORMULA: C14H16BNO
MW: 225.1
CAS NUMBER: 524-95-8
RTECS: ED6150000
PURITY: ≥98%
APPEARANCE: White crystalline solid.
SOLUBILITY: Soluble in DMSO, dimethyl formamide or 100% ethanol; also soluble in PBS, pH 7.2.
SHIPPING: SHIPPED ON BLUE ICE
LONG TERM STORAGE: -20°C
USE/STABILITY: Stable for at least 1 year after receipt when stored at -20°C. Stock solutions are stable for 2 months at -20°C.
HANDLING: After reconstitution, prepare aliquots and store at -20°C. Hygroscopic. Packaged under inert gas.

Product Description
Cell permeable modulator of Ins(1,4,5)-P3-induced Ca2+ release. A prototype drug for a group of structurally related calcium channel blockers in human platelets. Has been shown, in the absence of other stimuli, to activate TRPV1, V2 and V3, but not TRPV4, V5 and V6 expressed in HEK 293 cells.
Product Specific Literature References
2APB, 2-aminoethoxydiphenyl borate, a membrane-penetrable modulator of Ins(1,4,5)P3-induced Ca2+ release: T. Maruyama, et al.; J. Biochem. 122, 498 (1997) Abstract
Inhibition of SERCA Ca2+ pumps by 2-aminoethoxydiphenyl borate (2-APB). 2-APB reduces both Ca2+ binding and phosphoryl transfer from ATP, by interfering with the pathway leading to the Ca2+-binding sites: J.G. Bilmen, et al.; Eur. J. Biochem. 269, 3678 (2002) Abstract
2-aminoethoxydiphenyl borate (2-APB) is a reliable blocker of store-operated Ca2+ entry but an inconsistent inhibitor of InsP3-induced Ca2+ release: M.D. Bootman, et al.; FASEB J. 16, 1145 (2002) Abstract
Activation of TRPV4 channels (hVRL-2/mTRP12) by phorbol derivatives: H. Watanabe, et al.; J. Biol. Chem. 277, 13569 (2002) Abstract
2-Aminoethoxydiphenyl borate is a common activator of TRPV1, TRPV2 and TRPV3: H.Z. Hu, et al.; J. Biol. Chem. 279, 35741 (2004) Abstract; Full Text
TRPV4 calcium entry channel: a paradigm for gating diversity: B. Nilius, et al.; Am. J. Physiol. Cell Physiol. 286, C195 (2004) Abstract
2APB- and JTV519(K201)-sensitive micro Ca2+ waves in arrhythmogenic Purkinje cells that survive in infarcted canine heart: P.A. Boyden, et al.; Heart Rhythm 1, 218 (2004) Abstract
Inhibition of glutamate-induced delayed calcium deregulation by 2-APB and La3+ in cultured cortical neurones: C. Chinopoulos, et al.; J. Neurochem. 91, 471 (2004) Abstract
2-aminoethoxydiphenyl borate activates and sensitizes the heat-gated ion channel TRPV3: M.K. Chung, et al.; J. Neurosci. 24, 5177 (2004) Abstract; Full Text
The blocking of capacitative calcium entry by 2-aminoethyl diphenylborate (2-APB) and carboxyamidotriazole (CAI) inhibits proliferation in Hep G2 and Huh-7 human hepatoma cells: A. Enfissi, et al.; Cell Calcium 36, 459 (2004) Abstract
Induction of cholestasis in the perfused rat liver by 2-aminoethyl diphenylborate, an inhibitor of the hepatocyte plasma membrane Ca2+ channels: R.B. Gregory, et al.; J. Gastroenterol. Hepatol. 19, 1128 (2004) Abstract
2-aminoethoxydiphenyl borate inhibits agonist-induced Ca2+ signals by blocking inositol trisphosphate formation in acutely dissociated mouse pancreatic acinar cells: J. Wu, et al.; Pflugers Arch. 448, 592 (2004) Abstract
2-aminoethoxydiphenyl borate stimulates pulmonary C neurons via the activation of TRPV channels: Q. Gu, et al.; Am. J. Physiol. Lung Cell Mol. Physiol. 288, L392 (2005) Abstract
2-Aminoethoxydiphenyl borate perturbs hormone-sensitive calcium stores and blocks store-operated calcium influx pathways independent of cytoskeletal disruption in human A549 lung cancer cells: S. Padar, et al.; Biochem. Pharmacol. 69, 1177 (2005) Abstract
Block of TRPC5 channels by 2-aminoethoxydiphenyl borate: a differential, extracellular and voltage-dependent effect: S.Z. Xu, et al.; Br. J. Pharmacol. 145, 405 (2005) Abstract; Full Text
2-Aminoethoxydiphenyl borate (2-APB) stimulates a conformationally coupled calcium release pathway in the NG115-401L neuronal cell line: D.D. Bose & D.W. Thomas; Neuropharmacology 50, 532 (2006) Abstract
2-aminoethoxydiphenyl borate as a prototype drug for a group of structurally related calcium channel blockers in human platelets: Y. Dobrydneva, et al.; Mol. Pharmacol. 69, 247 (2006) Abstract
Further Categories Containing This Product:
TRPV2, TRPV3, TRPV4 / Related Products • TRPV1 Agonists and Antagonists / Related Products • TRP Channels Other Products
 
 
ALX-385-021 Revised 23-Oct-07
4'-Amino-6-hydroxyflavone
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SYNONYMS Aminogenistein
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Flavones
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ALX-385-021-M001   1 mg 140.00 USD Add To Cart
Product Specification
FORMULA: C15H11NO3
MW: 253.3
PURITY: ≥95%
APPEARANCE: Yellow powder.
SOLUBILITY: Soluble in DMSO or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Protect from light.

Product Description
Inhibitor of the p56lck protein-tyrosine kinase.
Product Specific Literature References
Synthesis and protein-tyrosine kinase inhibitory activities of flavonoid analogues: M. Cushman, et al.; J. Med. Chem. 34, 798 (1991) Abstract
Expression of p56lck in B-cell neoplasias: A. Von Knethen, et al.; Leuk. Lymphoma 26, 551 (1997) Abstract
Further Categories Containing This Product:
Tyrosine Kinase Inhibitors • Src Family Kinases / Related Products • Kinases in T Cell Signal Transduction / Related Products