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ALX-550-383
Revised 11-Apr-07
AM 1241
SYNONYMS
(2-Iodo-5-nitrophenyl)-(1-(1-methylpiperidin-2-ylmethyl)-1H-indol-3-yl)methanone
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Cannabinoid Receptor Agonists & Antagonists/Related Products
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Format:
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ALX-550-383-M001
1 mg
40.00 USD
ALX-550-383-M005
5 mg
110.00 USD
Product Specification
FORMULA:
C
22
H
22
N
3
O
3
I
MW:
503.3
PURITY:
≥97% (TLC)
APPEARANCE:
Yellow powder.
SOLUBILITY:
Soluble in DMSO, dimethyl formamide, 100% ethanol or methanol; insoluble in water.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Unstable in 1M NaOH; slightly unstable in 1M HCl.
HANDLING:
Packaged under inert gas. Protect from light.
Product Description
Potent and selective CB
2
receptor agonist (K
i
=3.4nM (mouse), K
i
=280nM (rat) also
in vivo
.
Product Specific Literature References
CB2 cannabinoid receptor-mediated peripheral antinociception
:
T.P. Malan, Jr., et al.; Pain
93
, 239 (2001)
Abstract
Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain: pain inhibition by receptors not present in the CNS
:
M.M. Ibrahim, et al.; PNAS
100
, 10529 (2003)
Abstract
;
Full Text
Selective activation of cannabinoid CB(2) receptors suppresses spinal fos protein expression and pain behavior in a rat model of inflammation
:
A.G. Nackley, et al.; Neuroscience
119
, 747 (2003)
Abstract
Inhibition of inflammatory hyperalgesia by activation of peripheral CB2 cannabinoid receptors
:
A. Quartilho, et al.; Anesthesiology
99
, 955 (2003)
Abstract
Selective activation of cannabinoid CB2 receptors suppresses hyperalgesia evoked by intradermal capsaicin
:
A.G. Hohmann, et al.; J. Pharmacol. Exp. Ther.
308
, 446 (2004)
Abstract
In vitro pharmacological characterization of AM1241: a protean agonist at the cannabinoid CB2 receptor?:
B.B. Yao, et al.; Br. J. Pharmacol.
149
, 145 (2006)
Abstract
ALX-260-003
Revised 09-May-07
Amastatin . hydrochloride
SYNONYMS
[(2S,3R)-3-Amino-2-hydroxy-5-methyl-hexanoyl]-Val-Val-Asp-OH . HCl
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Aminopeptidases/Related Products
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ALX-260-003-M001
1 mg
73.00 USD
ALX-260-003-M005
5 mg
235.00 USD
Product Specification
FORMULA:
C
21
H
38
N
4
O
8
. HCl
MW:
474.6 . 36.5
CAS NUMBER:
100938-10-1
SOURCE/HOST:
Synthetic.
PURITY:
≥98%
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in acetic acid.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Competitive inhibitor of human serum aminopeptidase A, pig kidney leucine aminopeptidase, leucine aminopeptidase, tyrosine aminopeptidase, but not of aminopeptidase B. Has been used to potentiate the action of some bioactive peptides by inhibiting their degradation by aminopeptidases.
Product Specific Literature References
Amastatin, an inhibitor of aminopeptidase A, produced by actinomycetes:
T. Aoyagi, et al.; J. Antibiot. (Tokyo)
31
, 636 (1978)
Abstract
H. Tobe, et al.; Agric. Biol. Chem.
43
, 591 (1979)
Inhibition of aminopeptidases by amastatin and bestatin derivatives. Effect of inhibitor structure on slow-binding processes:
D.H. Rich, et al.; J. Med. Chem.
27
, 417 (1984)
Abstract
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
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ALX-550-212-G001
1 g
23.00 USD
Product Specification
FORMULA:
C
6
H
8
ClN
7
O . 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 Ca
2+
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
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
Product Specification
FORMULA:
C
8
H
12
ClN
7
O . 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 (IC
50
=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)-
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
Product Specification
FORMULA:
C
11
H
18
ClN
7
O
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)-
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
Product Specification
FORMULA:
C
11
H
18
ClN
7
O
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
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
Product Specification
FORMULA:
C
6
H
9
NO
4
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
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
Product Specification
FORMULA:
C
6
H
9
NO
4
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
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
Product Specification
FORMULA:
C
6
H
11
NO
2
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
SYNONYMS
ACPC
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
NMDA Receptors/Related Products
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ALX-550-211-M050
50 mg
40.00 USD
Product Specification
FORMULA:
C
4
H
7
NO
2
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
SYNONYMS
2-APB
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Ca2+ Modulators
Ordering Information
