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Calcium Signalling (Intracellular)
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ALX-450-001 Revised 23-Jul-08
A23187 (free acid)
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SYNONYMS Calcium Ionophore A23187
Calcimycin
Antibiotic A23187
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-450-001-M001   1 mg 28.00 USD Add To Cart
ALX-450-001-M005   5 mg 65.00 USD Add To Cart
ALX-450-001-5001   5x1 mg 80.00 USD Add To Cart
ALX-450-001-M010   10 mg 92.00 USD Add To Cart
ALX-450-001-M025   25 mg 195.00 USD Add To Cart
ALX-450-001-M050   50 mg 350.00 USD Add To Cart
Product Specification
FORMULA: C29H37N3O6
MW: 523.6
CAS NUMBER: 52665-69-7
MERCK INDEX: 14: 1639
RTECS: DM4676000
SOURCE/HOST: Isolated from Streptomyces chartreusis.
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methylene chloride; slightly soluble in water. Solubilize in DMSO or ethanol prior to preparing aqueous solutions of very low concentrations.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
USE/STABILITY: In aqueous systems product may aggregate over time.
HANDLING: Protect from light. In aqueous systems, the product aggregates over time.
HAZARD: IRRITANT.

Product Description
Antibiotic possessing weak in vitro antimicrobial activity against gram positive bacteria and fungi. Divalent cation ionophore commonly used to increase intracellular Ca2+ levels in intact cells.
Product Specific Literature References
A23187: a divalent cation ionophore: P. W. Reed & H. A. Lardy; J. Biol. Chem. 247, 6970 (1972) Abstract
Effects of antibiotic ionophore, A23187, on oxidative phosphorylation and calcium transport of liver mitochondria: D.T. Wong, et al.; Arch. Biochem. Biophys. 156, 578 (1973) Abstract
Biological applications of ionophores: B.C. Pressman; Annu. Rev. Biochem. 45, 501 (1976), (Review) Abstract
Molecular mechanisms of endothelium-mediated vasodilation: R.R. Fiscus; Semin. Thromb. Hemost. 14 Suppl, 12 (1988), (Review) Abstract
Calcium ionophore A23187 action on cardiac myocytes is accompanied by enhanced production of reactive oxygen species: 1740, 481 (2005): T. Przygodzki, et al.; Biochim. Biophys. Acta 1740, 481 (2005) Abstract
Further Categories Containing This Product:
Nitric Oxide Pathway Other Products • Respiratory Chain Other Products • Antibiotics - ATPase Inhibitors
 
 
ALX-450-002 Revised 14-Nov-07
A23187 (Mixed Calcium-Magnesium Salt)
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-450-002-M005   5 mg 60.00 USD Add To Cart
ALX-450-002-M010   10 mg 110.00 USD Add To Cart
ALX-450-002-M050   50 mg 415.00 USD Add To Cart
Product Specification
MERCK INDEX: 13: 1639
SOURCE/HOST: Semisynthetic.
PURITY: ≥98% (molar ratio Ca:Mg ~1:1)
APPEARANCE: White solid.
SOLUBILITY: Soluble in methylene chloride, chloroform, acetone, ethyl acetate, or diethyl ketone; also soluble in DMSO, 100% ethanol, and ethanol. Solubilize in DMSO or ethanol prior to preparing aqueous solutions of very low concentrations.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HANDLING: Protect from light. In aqueous systems, product may aggregate over time.
HAZARD: TOXIC.

Product Description
Salt form of A23187 (Prod. No. ALX-450-001). Used in cell activation experiments when calcium dose-response data are not required.
 
 
ALX-630-001 Revised 10-Oct-08
ω-Agatoxin IVA
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PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Neurotoxins
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ALX-630-001-C100   100 µg 580.00 USD Add To Cart
Product Specification
SEQUENCE: H-Lys-Lys-Lys-Cys-Ile-Ala-Lys-Asp-Tyr-Gly-Arg-Cys-Lys-Trp-Gly-Gly-Thr-Pro-Cys-Cys-Arg-Gly-Arg-Gly-Cys-Ile-Cys-Ser-Ile-Met-Gly-Thr-Asn-Cys-Glu-Cys-Lys-Pro-Arg-Leu-Ile-Met-Glu-Gly-Leu-Gly-Leu-Ala-OH
(Disulfide bonds between Cys4-Cys20, Cys12-Cys25, Cys19-Cys36 and Cys27-Cys34)
FORMULA: C217H360N68O60S10
MW: 5202.3
CAS NUMBER: 145017-83-0
RTECS: AW8050000
SOURCE/HOST: Synthetic. Originally isolated from Agelenopsis aperta.
PURITY: ≥98%
APPEARANCE: Lyophilized.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HAZARD: HARMFUL.
Product Description
Selective P-type Ca2+ channel blocker. Fast acting and potent eurotoxin.
Product Specific Literature References
P-type calcium channels blocked by the spider toxin omega-Aga-IVA: I.M. Mintz, et al.; Nature 355, 827 (1992) Abstract
Calcium channels coupled to glutamate release identified by omega-Aga- IVA: T.J. Turner, et al.; Science 258, 310 (1992) Abstract
Synthesis of omega-agatoxin IVA and its related peptides: H. Nishio, et al.; BBRC 196, 1447 (1993) Abstract
Interactions of polyamines with neuronal ion channels: R.H. Scott, et al.; TINS 16, 153 (1993), (Review) Abstract
Different types of calcium channels mediate central synaptic transmission: T. Takahashi & A. Momiyama; Nature 366, 156 (1993) Abstract
Sequential assignment and structure determination of spider toxin omega- Aga-IVB: H. Yu, et al.; Biochemistry 32, 13123 (1993) Abstract
Calcium channel diversity and neurotransmitter release: the omega-conotoxins and omega-agatoxins: B.M. Olivera, et al.; Ann. Rev. Biochem. 63, 823 (1994) Abstract
Exocytotic Ca2+ channels in mammalian central neurons: K. Dunlap, et al.; TINS 18, 89 (1995), (Review) Abstract
P/Q-type Ca2+ channel blocker omega-agatoxin IVA protects against brain injury after focal ischemia in rats: K. Asakura, et al.; Brain Res. 776, 140 (1997) Abstract
Agatoxin-IVA-sensitive calcium channels mediate the presynaptic and postsynaptic nicotinic activation of cardiac vagal neurons: J. Wang, et al.; J. Neurophysiol. 85, 164 (2001) Abstract
Further Categories Containing This Product:
Ca2+ Channels (P / Q-type)
 
 
ALX-380-046 Revised 08-Apr-08
Alamethicin
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SYNONYMS U-22324
PRODUCT LINE Natural Products / Antibiotics
PRODUCT CATEGORY Antibiotics - Ionophores
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ALX-380-046-M001   1 mg 40.00 USD Add To Cart
ALX-380-046-M005   5 mg 90.00 USD Add To Cart
Product Specification
SEQUENCE: Main component: Ac-Aib-Pro-Aib-Ala-Aib-Ala-Gln-Aib-Val-Aib-Gly-Leu-Aib-Pro-Val-Aib-Aib-Glu-Gln-Phl
FORMULA: C92H150N22O25
MW: 1964.3
CAS NUMBER: 27061-78-5, 59588-86-2
SOURCE/HOST: Isolated from Trichoderma viride.
PURITY: ≥50% (remainder homologs)
APPEARANCE: Off-white to brown solid.
SOLUBILITY: Soluble in DMSO, 100% ethanol or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
USE/STABILITY: Solutions are stable for up to 3 months when stored at -20°C.
HAZARD: TOXIC.
Product Description
Membrane permeabilizing antibiotic.
Product Specific Literature References
The primary structure of alamethicin: J.W. Payne, et al.; Biochem. J. 117, 757 (1970) Abstract
Alamethicin-mediated fusion of lecithin vesicles: A.L.Y. Lau and S.I. Chan; PNAS 72, 2170 (1975) Abstract
The use of ionophores and channel formers in the study of the function of biological membranes: A. Gomez-Puyou & C. Gomez-Lojero; Curr. Top. Bioener. 6, 221 (1977)
The production of alamethicins by Trichoderma spp: D. Brewer, et al.; Can. J. Microbiol. 33, 619 (1987) Abstract
Model ion channels: gramicidin and alamethicin: G. A. Woolley & B. A. Wallace; J. Membr. Biol. 129, 109 (1992), Review Abstract
Ligand-induced extramembrane conformation switch controlling alamethicin assembly and the channel current: S. Futaki & K. Asami; Chem. Biodivers. 4, 1313 (2007), Review Abstract
Channel-forming activity of alamethicin: effects of covalent tethering: G.A. Woolley; Chem. Biodivers. 4, 1323 (2007), Review Abstract
 
 
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-400-045 Revised 31-Aug-07
2-Aminoethoxydiphenyl borate
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SYNONYMS 2-APB
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Ca2+ Modulators
Ordering Information
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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