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Imidazoline Binding Site Ligands
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ALX-550-001 Revised 20-Jun-07
Agmatine . sulfate
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SYNONYMS 1-Amino-4-guanidinobutane . sulfate
4-(Aminobutyl)guanidine . sulfate
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Imidazoline Binding Site Ligands
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Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-550-001-M100   100 mg 22.00 USD Add To Cart
ALX-550-001-M500   500 mg 44.00 USD Add To Cart
Product Specification
FORMULA: C5H14N4 . H2SO4
MW: 130.2 . 98.1
CAS NUMBER: 2482-00-0
MERCK INDEX: 14: 188
PURITY: ≥97%
APPEARANCE: White to off-white powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C

Product Description
Decarboxylation product of L-arginine. Endogenous clonidine-displacing substance in the brain. Putative endogenous neurotransmitter at imidazoline receptors. Antagonist of NMDA receptor. Endogenous inhibitor of nitric oxide synthase (NOS). Antiproliferative by its suppresive effect on polyamine.
Product Specific Literature References
Agmatine: an endogenous clonidine-displacing substance in the brain: G. Li, et al.; Science 263, 966 (1994) Abstract
Selective inhibition of inducible nitric oxide synthase by agmatine: M. Auguet, et al.; Jpn. J. Pharmacol. 69, 285 (1995) Abstract
Inhibition of mammalian nitric oxide synthases by agmatine, an endogenous polyamine formed by decarboxylation of arginine: E. Galea, et al.; Biochem. J. 316, 247 (1996) Abstract; Full Text
An emerging role for agmatine: J. Satriano, et al.; Kidney Int. 56, 1252 (1999), (Review) Abstract
Is agmatine a novel neurotransmitter in brain?: D.J. Reis & S. Regunathan; Trends Pharmacol. Sci. 21, 187 (2000) Abstract
Agmatine suppresses nitric oxide production in microglia: K. Abe, et al.; Brain Res. 872, 141 (2000) Abstract
Agmatine enhances the NADPH oxidase activity of neuronal NO synthase and leads to oxidative inactivation of the enzyme: D.R. Demady, et al.; Mol. Pharmacol. 59, 24 (2001) Abstract; Full Text
Regulation of inducible nitric oxide synthase and agmatine synthesis in macrophages and astrocytes: S. Regunathan & J.E. Piletz; Ann. N. Y. Acad. Sci. 1009, 20 (2003) Abstract
Agmatine: at the crossroads of the arginine pathways: J. Satriano; Ann. N. Y. Acad. Sci. 1009, 34 (2003), (Review) Abstract
Agmatine signaling: odds and threads: R. Berkels, et al.; Cardiovasc. Drug Rev. 22, 7 (2004), (Review) Abstract
Further Categories Containing This Product:
NMDA Receptors / Related Products • NOS Inhibitors (NOS Induction & Enzyme Activity)
 
 
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
Ordering Information
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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-550-162 Revised 12-May-03
2-(2-Benzofuranyl)-2-imidazoline . hydrochloride
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SYNONYMS 2-BFI . HCl
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Imidazoline Binding Site Ligands
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ALX-550-162-M001   1 mg 25.00 USD Add To Cart
ALX-550-162-M005   5 mg 70.00 USD Add To Cart
Product Specification
FORMULA: C11H10N2O . HCl
MW: 186.2 . 36.5
CAS NUMBER: 89196-95-2
PURITY: ≥95%
APPEARANCE: White powder.
SOLUBILITY: Soluble in water.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C

Product Description
Highly selective I2 ligand.
Product Specific Literature References
[3H]2-(2-benzofuranyl)-2-imidazoline: a new selective high affinity radioligand for the study of rabbit brain imidazoline I2 receptors: L.A. Lione, et al.; Eur. J. Pharmacol. 304, 221 (1996) Abstract
[3H]2-(2-Benzofuranyl)-2-imidazoline, a highly selective radioligand for I2-imidazoline receptor binding sites. Studies in rabbit kidney membranes: A.R. Hosseini, et al.; Naunyn-Schmiedeberg's Arch. Pharmacol. 355, 131 (1997) Abstract
Labelling of I2B-imidazoline receptors by [3H]2-(2-benzofuranyl)-2-imidazoline (2-BFI) in rat brain and liver: characterization, regulation and relation to monoamine oxidase enzymes: R. Alemany, et al.; Naunyn-Schmiedeberg's Arch. Pharmacol. 356, 39 (1997) Abstract
Activation of I(2)-imidazoline receptors enhances supraspinal morphine analgesia in mice: a model to detect agonist and antagonist activities at these receptors: P. Sanchez-Blazquez, et al.; Br. J. Pharmacol. 130, 146 (2000) Abstract
 
 
ALX-550-087 Revised 15-Sep-08
Clonidine . hydrochloride
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SYNONYMS
2-(2,6-Dichloroanilino)-2-imidazoline . hydrochloride
PRODUCT LINE Neurobiology
PRODUCT CATEGORY Adrenergics & Adrenergic Receptors / Related Products
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ALX-550-087-M050   50 mg 23.00 USD Add To Cart
Product Specification
FORMULA: C9H9Cl2N3 . HCl
MW: 230.1 . 36.5
CAS NUMBER: 4205-91-8
MERCK INDEX: 14: 2390
RTECS: NJ2490000
PURITY: ≥98% (HPLC)
APPEARANCE: White to off-white solid.
SOLUBILITY: Soluble in water (50mg/ml) or methanol.
SHIPPING: AMBIENT
LONG TERM STORAGE: +4°C
HAZARD: VERY TOXIC.

Product Description
α2-Adrenergic receptor agonist. Antihypertensive.
Further Categories Containing This Product:
Imidazoline Binding Site Ligands
 
 
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