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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
Ordering Information
Product Numbers:
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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-550-213
Revised 06-Jun-08
(±)-BAY K 8644
SYNONYMS
1,4-Dihydro-2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)-phenyl]pyridine-3-carboxylic acid methyl ester
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Ca2+ Channels (L-type)
Ordering Information
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ALX-550-213-M005
5 mg
80.00 USD
ALX-550-213-M025
25 mg
320.00 USD
Product Specification
FORMULA:
C
16
H
15
F
3
N
2
O
4
MW:
356.3
CAS NUMBER:
93468-89-4
PURITY:
≥98% (HPLC)
APPEARANCE:
Yellow powder.
SOLUBILITY:
Soluble in DMSO, 100% ethanol or methanol; slightly soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
Potent, direct acting, voltage-sensitive Ca
2+
channel (L-type) agonist.
Product Specific Literature References
The optical isomers of the 1,4-dihydropyridine BAY K 8644 show opposite effects on Ca channels:
G. Franckowiak, et al.; Eur. J. Pharmacol.
114
, 223 (1985)
Abstract
BAY-K-8644, a calcium channel agonist, induces a rise in cytoplasmic free calcium and iodide discharge in thyroid cells:
N. Takasu, et al.; BBRC
143
, 1107 (1987)
Abstract
Goldstein, et al.; Drug Dev. Res.
11
, 59 (1987)
Calcium channel ligands:
D.J. Triggle & R.A. Janis; Ann. Rev. Pharmacol. Toxicol.
27
, 347 (1987)
Abstract
1,4-Dihydropyridine activators and antagonists: structural and functional distinctions:
D.J. Triggle & D. Rompe; TIPS
10
, 507 (1989)
Abstract
ALX-550-214
Revised 03-Feb-05
Diltiazem . hydrochloride
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Ca2+ Channels (L-type)
Ordering Information
Product Numbers:
Format:
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Unit Price:
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ALX-550-214-G001
1 g
40.00 USD
ALX-550-214-G005
5 g
110.00 USD
Product Specification
FORMULA:
C
22
H
26
N
2
O
4
S . HCl
MW:
414.5 . 36.5
CAS NUMBER:
33286-22-5
MERCK INDEX:
14:
3202
PURITY:
≥99%
APPEARANCE:
White powder.
SOLUBILITY:
Soluble in water, methanol or chloroform.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+20°C
Product Description
Inhibitor of L-type Ca
2+
channels. Regulates Ca
2+
release from intracellular stores in neutrophils.
Product Specific Literature References
Diltiazem. A review of its pharmacological properties and therapeutic efficacy:
M. Chaffman & R.N. Bogden; Drugs
29
, 387 (1985)
Abstract
ALX-550-216
Revised 06-Jul-06
Tolazamide
SYNONYMS
U-17835
N-[[(Hexahydro-1
H
-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
ALX-550-216-G005
5 g
35.00 USD
Product Specification
FORMULA:
C
14
H
21
N
3
O
3
S
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
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
ALX-550-222-M250
250 mg
80.00 USD
Product Specification
FORMULA:
C
23
H
31
NO
2
. 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) (IC
50
=90µM). Inhibitor of cytochrome P450 system. Calcium antagonist. Blocks glibenclamide-sensitive K
+
channels (IC
50
=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:
Cytochrome P450 [CYP450] / Related Products
•
K+ Channel Blockers & Inhibitors
ALX-550-228
Revised 30-May-06
5-Nitro-6,7-dichloro-1,4-dihydro-2,3-quinoxalinedione
SYNONYMS
ACEA-1021
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
NMDA Receptors / Related Products
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ALX-550-228-M005
5 mg
90.00 USD
ALX-550-228-M025
25 mg
360.00 USD
Product Specification
FORMULA:
C
8
H
3
Cl
2
N
3
O
4
MW:
276.0
PURITY:
≥98%
APPEARANCE:
Yellow powder.
SOLUBILITY:
Soluble in DMSO or dilute aqueous base.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
Potent and selective NMDA receptor glycine site antagonist.
Product Specific Literature References
Synthesis and structure-activity relationships of substituted 1,4- dihydroquinoxaline-2,3-diones: antagonists of N-methyl-D-aspartate (NMDA) receptor glycine sites and non-NMDA glutamate receptors:
J.F.W. Keana, et al.; J. Med. Chem.
38
, 4367 (1995)
Abstract
In vitro pharmacology of ACEA-1021 and ACEA-1031: systemically active quinoxalinediones with high affinity and selectivity for N-methyl-D- aspartate receptor glycine sites:
R.M. Woodward, et al.; Mol. Pharmacol.
47
, 568 (1995)
Abstract
Pharmacology of 5-chloro-7-trifluoromethyl-1,4-dihydro-2,3- quinoxalinedione: a novel systemically active ionotropic glutamate receptor antagonist:
R.M. Woodward, et al.; J. Pharmacol. Exp. Ther.
275
, 1209 (1995)
Abstract
ALX-550-229
Revised 11-Nov-05
FPL 64176
SYNONYMS
2,5-Dimethyl-4-[2-(phenylmethyl)benzoyl]-1H-pyrrole-3-carboxylic acid methyl ester
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Ca2+ Channels (L-type)
Ordering Information
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ALX-550-229-M005
5 mg
70.00 USD
Product Specification
FORMULA:
C
22
H
21
NO
3
MW:
347.4
CAS NUMBER:
120934-96-5
PURITY:
≥99%
APPEARANCE:
White to tan powder.
SOLUBILITY:
Soluble in 100% ethanol or DMSO; insoluble in aqueous solution.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Hygroscopic. Protect from light.
Product Description
Potent Ca
2+
channel (L-type) activator.
Product Specific Literature References
A new site for the activation of cardiac calcium channels defined by the nondihydropyridine FPL 64176:
D. Rampe & A.E. Lacerda; J. Pharmacol. Exp. Ther.
259
, 982 (1991)
Abstract
Pharmacological, radioligand binding, and electrophysiological characteristics of FPL 64176, a novel nondihydropyridine Ca2+ channel activator, in cardiac and vascular preparations:
W. Zheng, et al.; Mol. Pharmacol.
40
, 734 (1991)
Abstract
Comparison of the in vitro and in vivo cardiovascular effects of two structurally distinct Ca++ channel activators, BAY K 8644 and FPL 64176:
D. Rampe, et al.; J. Pharmacol. Exp. Ther.
265
, 1125 (1993)
Abstract
ALX-550-231
Revised 13-Aug-04
(R)-CPP
SYNONYMS
3-((R)-2-Carboxypiperazin-4-yl)-propyl-1-phosphonic acid
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
NMDA Receptors / Related Products
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ALX-550-231-M001
1 mg
35.00 USD
Product Specification
FORMULA:
C
8
H
17
N
2
O
5
P
MW:
252.2
CAS NUMBER:
126453-07-4
PURITY:
≥97%
APPEARANCE:
White crystalline powder.
SOLUBILITY:
Soluble in dilute aqueous base or water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+20°C
Product Description
Highly potent NMDA receptor antagonist.
Product Specific Literature References
CPP, a new potent and selective NMDA antagonist. Depression of central neuron responses, affinity for [3H]D-AP5 binding sites on brain membranes and anticonvulsant activity
:
J. Davies, et al.; Brain Res.
382
, 169 (1986)
Abstract
Synthesis and NMDA antagonistic properties of the enantiomers of 4-(3-phosphonopropyl)piperazine-2-carboxylic acid (CPP) and of the unsaturated analogue (E)-4-(3-posphonoprop2-enyl)piperazine-2-carboxylic acid (CPP-ene)
:
B. Aebischer, et al.; Helv. Chim. Acta
72
, 1043 (1989)
ALX-550-232
Revised 13-May-08
Aconitine
SYNONYMS
(1α,3α,6α,14α,15α,16β)-20-Ethyl-1,6,16-trimethoxy-4-(methoxymethyl)aconitane-3,8,13,14,15-pentol 8-acetate 14-benzoate
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Neurotoxins
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ALX-550-232-M025
25 mg
45.00 USD
Product Specification
FORMULA:
C
34
H
47
NO
11
MW:
645.7
CAS NUMBER:
302-27-2
MERCK INDEX:
14:
118
RTECS:
AR5960000
SOURCE/HOST:
Isolated from
Aconitum karacolium
.
PURITY:
≥98%
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in 100% ethanol (35mg/ml); almost insoluble in water (0.3mg/ml).
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Protect from light.
HAZARD:
VERY TOXIC.
Product Description
A lipid-soluble neurotoxin that acts as a sodium channel modulator. Blocks tetrodotoxin-sensitive Na
+
channels. Potent neurotoxin.
Product Specific Literature References
Non-quantal acetylcholine release at mouse neuromuscular junction: effects of elevated quantal release and aconitine:
S.P. Yu & W. Van der Kloot; Neurosci. Lett.
117
, 111 (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:
M. Muroi, et al.; Neuropharmacology
29
, 567 (1990)
Abstract
Further Categories Containing This Product:
Alkaloids
•
Na+ Channels
ALX-550-235
Revised 08-Aug-08
Benzamil . hydrochloride
SYNONYMS
Benzylamiloride . HCl
N-(Benzylamidino)-3,5-diamino-6-chloropyrazinecarboxamide . HCl
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Na+ Channels
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-550-235-M005
5 mg
25.00 USD
ALX-550-235-M025
25 mg
95.00 USD
Product Specification
FORMULA:
C
13
H
14
ClN
7
O . HCl
MW:
319.8 . 36.5
CAS NUMBER:
2898-76-2
PURITY:
≥98% (TLC)
APPEARANCE:
Yellow solid.
SOLUBILITY:
Soluble in water or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
USE/STABILITY:
Stock solutions are stable for up to 3 months when stored at -20°C.
HANDLING:
Protect from light.
HAZARD:
IRRITANT.
Product Description
Derivative of amiloride (Prod. No.
ALX-550-212
). Potent Na
+
channel blocker.
Product Specific Literature References
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
Structure-activity relations of amiloride and its analogues in blocking the mechanosensitive channel in Xenopus oocytes:
J.W. Lane, et al.; Br. J. Pharmacol.
106
, 283 (1992)
Abstract
Modulation of cardiac performance by amiloride and several selected derivatives of amiloride:
G.N. Pierce, et al.; J. Pharmacol. Exp. Ther.
265
, 1280 (1993)
Abstract
ALX-550-237
Revised 18-Jan-05
Bepridil . hydrochloride
SYNONYMS
1-Isobutoxy-2-pyrrolidino-3-(N-benzylanilino)propane . HCl
PRODUCT LINE
