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Items 15 of 15
ALX-270-022
Revised 09-Jan-08
AEBSF . hydrochloride
SYNONYMS
4-(2-Aminoethyl)benzenesulfonylfluoride . HCl
Pefabloc
®
SC
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Proteases Other Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-270-022-M050
50 mg
40.00 USD
ALX-270-022-M250
250 mg
145.00 USD
ALX-270-022-G001
1 g
360.00 USD
Product Specification
FORMULA:
C
8
H
10
FNO
2
S . HCl
MW:
203.2 . 36.5
CAS NUMBER:
30827-99-7
PURITY:
≥98% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in water or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Protect from moisture.
Product Description
Specific irreversible inhibitor of serine proteases including trypsin, chymotrypsin, plasmin, plasma kallikrein, and thrombin. Stable, non-toxic alternative to PMSF (Prod. No.
ALX-270-184
). Inhibitor of NAD(P)H oxidase. Activator of MAP kinases JNK and p38.
Product Specific Literature References
Irreversible enzyme inhibitors. 180. Irreversible inhibitors of the C'la component of complement derived from m-(phenoxypropoxy)benzamidine and phenoxyacetamide:
B.R. Baker & H.J. Cory; J. Med. Chem.
14
, 119 (1971)
Abstract
Serine protease inhibitors block priming of monocytes for enhanced release of superoxide:
P. Megyeri, et al.; Immunology
86
, 629 (1995)
Abstract
;
Full Text
Inhibition of amyloid beta-protein production in neural cells by the serine protease inhibitor AEBSF:
M. Citron, et al.; Neuron
17
, 171 (1996)
Abstract
Lysis of leukemic cells by human macrophages: inhibition by 4-(2-aminoethyl)-benzenesulfonyl fluoride (AEBSF), a serine protease inhibitor:
Y. Nakabo & M.J. Pabst; J. Leukoc. Biol.
60
, 328 (1996)
Abstract
;
Full Text
Inhibition of NADPH oxidase activation by 4-(2-aminoethyl)-benzenesulfonyl fluoride and related compounds:
V. Diatchuk, et al.; J. Biol. Chem.
272
, 13292 (1997)
Abstract
;
Full Text
4-(2-Aminoethyl)benzenesulfonyl fluoride attenuates tumor-necrosis-factor-alpha-induced blood-brain barrier opening:
P. Megyeri, et al.; Eur. J. Pharmacol.
374
, 207 (1999)
Abstract
Evaluation of two inhibitors of invasion: LY311727 [3-(3-acetamide-1-benzyl-2-ethyl-indolyl-5-oxy)propane phosphonic acid] and AEBSF [4-(2-aminoethyl)-benzenesulphonyl fluoride] in acute murine toxoplasmosis:
R. Buitrago-Rey, et al.; J. Antimicrob. Chemother.
49
, 871 (2002)
Abstract
;
Full Text
Heme oxygenase-1 gene activation by the NAD(P)H oxidase inhibitor 4-(2-aminoethyl) benzenesulfonyl fluoride via a protein kinase B, p38-dependent signaling pathway in monocytes:
N. Wijayanti, et al.; J. Biol. Chem.
280
, 21820 (2005)
Abstract
;
Full Text
Inhibitory effect of 4-(2-aminoethyl)-benzenesulfonyl fluoride, a serine protease inhibitor, on PI3K inhibitor-induced CHOP expression:
T. Hosoi, et al.; Eur. J. Pharmacol.
554
, 8 (2007)
Abstract
Further Categories Containing This Product:
Heme Oxygenase / Related Products
•
Cell Stress, Oxidative Stress & Redox Signalling Other Products
•
MAPK Pathway Activators
•
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-340-055
Revised 21-Jul-08
N-Arachidonoyl glycine
SYNONYMS
NAGly
N-[1-Oxo-5Z,8Z,11Z,14Z-Eicosatetraenyl]-glycine
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Anandamide & Anandamide Analogs
Ordering Information
Product Numbers:
Format:
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ALX-340-055-M005
5 mg
55.00 USD
Product Specification
FORMULA:
C
22
H
35
NO
3
MW:
361.5
CAS NUMBER:
179113-91-8
CONCENTRATION:
50mg/ml
PURITY:
≥98%
FORMULATION:
Liquid. Solution in ethanol.
SOLUBILITY:
15mg/ml soluble in DMSO or dimethyl formamide; 2mg/ml soluble in
PBS (pH 7.2).
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stable for at least 2 years after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.
Product Description
Endogenous anandamide-like compound. Lacks affinity for CB
1
receptors (K
i
>10µM), TRPV1 (EC
50
>10µM) and anandamide uptake (IC
50
>50µM), but inhibits fatty acid amide hydrolase (FAAH) (IC
50
=8.5µM-50µM, depending on cell type and species).
Product Specific Literature References
Structural requirements for binding of anandamide-type compounds to the brain cannabinoid receptor
:
T. Sheskin, et al.; J. Med. Chem.
40
, 659 (1997)
Abstract
Identification of a new class of molecules, the arachidonyl amino acids, and characterization of one member that inhibits pain
:
S.M. Huang, et al.; J. Biol. Chem.
276
, 42639 (2001)
Abstract
A structure-activity relationship study on N-arachidonoyl-amino acids as possible endogenous inhibitors of fatty acid amide hydrolase
:
M. Grazia Cascio, et al.; BBRC
314
, 192 (2004)
Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION
To change the solvent, evaporate the ethanol under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Anandamide Uptake Inhibitors
•
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-340-060
Revised 10-Jul-08
Arachidonoyl serotonin
SYNONYMS
AA-5HT
N-[2-(5-Hydroxy-1
H
-indol-3-yl)]ethyl-5Z,8Z,11Z,14Z-eicosatetraenamide
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Anandamide & Anandamide Analogs
Ordering Information
Product Numbers:
Format:
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ALX-340-060-M005
5 mg
55.00 USD
Product Specification
FORMULA:
C
30
H
42
N
2
O
2
MW:
462.7
CAS NUMBER:
187947-37-1
PURITY:
≥98%
FORMULATION:
Liquid. Solution in methyl acetate.
SOLUBILITY:
Soluble in 100% ethanol (15mg/ml), DMSO (30mg/ml), dimethyl formamide (30mg/ml) or PBS, pH 7.2 (290μg/ml).
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. We do not recommend storing aqueous solutions for more than one day.
Product Description
Tight binding, competitive inhibitor of fatty acid amide hydrolase (FAAH) (IC
50
=12µM).
Product Specific Literature References
Arachidonoylserotonin and other novel inhibitors of fatty acid amide hydrolase
:
T. Bisogno, et al.; BBRC
248
, 515 (1998)
Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION
To change the solvent, evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-340-001
Revised 28-Jul-06
Arachidonyl trifluoromethylketone
SYNONYMS
AACOCF
3
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PLA2 Inhibitors
Ordering Information
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Format:
Size:
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ALX-340-001-M005
5 mg
70.00 USD
ALX-340-001-M010
10 mg
110.00 USD
ALX-340-001-M050
50 mg
390.00 USD
Product Specification
FORMULA:
C
21
H
31
F
3
O
MW:
356.5
CAS NUMBER:
149301-79-1
PURITY:
≥98%
APPEARANCE:
Clear to yellow oil.
SOLUBILITY:
25mg/ml soluble in 100% ethanol or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Dissolve in solvent purged with nitrogen or argon. Store under nitrogen or argon in tightly sealed container. Solutions are stable for up to 1 month when stored under nitrogen or argon in tightly sealed container at -80°C.
HANDLING:
PROTECT FROM AIR!
HAZARD:
TOXIC.
Product Description
Selective inhibitor of both, Ca
2+-
dependent and Ca
2+
-independent phospholipase A
2
(PLA
2
), but not secretory PLA
2
(sPLA
2
). Also inhibits fatty acid amide hydrolase (FAAH) and anandamide amidase.
Product Specific Literature References
Inhibitors of arachidonoyl ethanolamide hydrolysis:
B. Koutek, et al.; J. Biol. Chem.
269
, 22937 (1994)
Abstract
;
Full Text
Further Categories Containing This Product:
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-340-042
Revised 07-Jan-06
Arvanil
SYNONYMS
N-[(4-Hydroxy-3-methoxyphenyl)methyl]-5
Z
,8
Z
,11
Z
,14
Z
-eicosatetraenamide
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Cannabinoid Receptor Agonists & Antagonists / Related Products
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ALX-340-042-M005
5 mg
25.00 USD
Product Specification
FORMULA:
C
28
H
41
NO
3
MW:
439.6
CAS NUMBER:
128007-31-8
PURITY:
≥98%
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light. Keep cool and dry.
Product Description
"Hybrid" activator of CB
1
receptor (CB
1
: K
i
=0.5µM; CB
2
: K
i
=>15µM) and TRPV1 (K
i
=0.3µM). Also inhibits anandamide uptake (IC
50
=3.6µM) and fatty acid amide hydrolase (FAAH) (IC
50
=3µM). Analgesic, vasodilatory and anti-inflammatory
in vivo
. Apoptosis inducer.
Product Specific Literature References
Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid receptors:
D. Melck, et al.; BBRC
262
, 275 (1999)
Abstract
Neurobehavioral activity in mice of N-vanillyl-arachidonyl-amide
:
V. Di Marzo, et al.; Eur. J. Pharmacol.
406
, 363 (2000)
Abstract
A structure/activity relationship study on arvanil, an endocannabinoid and vanilloid hybrid
:
V. Di Marzo, et al.; J. Pharmacol. Exp. Ther.
300
, 984 (2002)
Abstract
The CB1/VR1 agonist arvanil induces apoptosis through an FADD/caspase-8-dependent pathway
:
R. Sancho, et al.; Br. J. Pharmacol.
140
, 1035 (2003)
Abstract
Evidence against the presence of an anandamide transporter
:
S.T. Glaser, et al.; PNAS
100
, 4269 (2003)
Abstract
Arvanil, a hybrid endocannabinoid and vanilloid compound, behaves as an antihyperkinetic agent in a rat model of Huntington's disease:
E. de Lago, et al.; Brain Res.
1050
, 210 (2005)
Abstract
Arvanil inhibits T lymphocyte activation and ameliorates autoimmune encephalomyelitis:
A.M. Malfitano, et al.; J. Neuroimmunol.
171
, 110 (2006)
Abstract
Further Categories Containing This Product:
Anandamide Uptake Inhibitors
•
Apoptosis Inducers & Inhibitors Other Products
•
TRPV1 Agonists and Antagonists / Related Products
•
Analgesic / Anti-nociceptive Agents / Related Products
•
Anti-inflammatory Agents Other Products
•
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-550-523
Revised 11-Apr-07
JP83
SYNONYMS
3’-Carbamoyl-biphenyl-3-yl-hexylphenylcarbamate
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Fatty Acid Amide Hydrolase [FAAH] / Related Products
Ordering Information
Product Numbers:
Format:
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ALX-550-523-M005
5 mg
40.00 USD
Product Specification
FORMULA:
C
26
H
28
N
2
O
3
MW:
416.5
PURITY:
≥98%
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in 100% ethanol, DMSO or dimethyl formamide; sparingly soluble in aqueous buffers.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stable for at least 2 years after receipt when stored at -20°C.
Product Description
Irreversible inhibitor of human fatty acid amide hydrolase (FAAH) (IC
50
=14nM), when tested using radiolabelled oleamide as the substrate.
Product Specific Literature References
Mechanism of carbamate inactivation of FAAH: implications for the design of covalent inhibitors and in vivo functional probes for enzymes:
J.P. Alexander and B.F. Cravatt; Chem. Biol.
12
, 1179 (2005)
Abstract
ALX-550-411
Revised 11-Apr-07
LY2183240
SYNONYMS
5-Biphenyl-4-ylmethyltetrazole-1-carboxylic acid dimethylamide
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Anandamide Uptake Inhibitors
Ordering Information
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Format:
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ALX-550-411-M010
10 mg
60.00 USD
ALX-550-411-M050
50 mg
240.00 USD
Product Specification
FORMULA:
C
17
H
17
N
5
O
MW:
307.4
CAS NUMBER:
874902-19-9
PURITY:
≥98% (TLC)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO or dimethyl formamide.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
Product Description
Initially described as potent, competitive small molecule inhibitor of anandamide uptake. Has recently been shown to inhibit fatty acid amide hydrolase (FAAH) and several additional serine hydrolases.
Product Specific Literature References
Identification of a high-affinity binding site involved in the transport of endocannabinoids:
S.A. Moore, et al.; PNAS
102
, 17852 (2005)
Abstract
;
Full Text
Toward an anandamide transporter:
R. Mechoulam and D.G. Deutsch; PNAS
102
, 17541 (2005)
Abstract
The putative endocannabinoid transport blocker LY2183240 is a potent inhibitor of FAAH and several other brain serine hydrolases:
J.P. Alexander and B.F. Cravatt; JACS
128
, 9699 (2006)
Abstract
Pharmacological characterization of endocannabinoid transport and fatty acid amide hydrolase inhibitors:
A.K. Dickason-Chesterfield, et al.; Cell. Mol. Neurobiol.
26
, 407 (2006)
Abstract
Further Categories Containing This Product:
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-340-017
Revised 11-Jul-08
Methylarachidonyl fluorophosphonate
SYNONYMS
MAFP
Methylphosphonofluoridic acid 5,8,11,14-eicosatetraenyl ester
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
PLA2 Inhibitors
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-340-017-M001
1 mg
33.00 USD
ALX-340-017-M005
5 mg
147.00 USD
Product Specification
FORMULA:
C
21
H
36
FO
2
P
MW:
370.5
CONCENTRATION:
10mg/ml
PURITY:
≥98%
FORMULATION:
Liquid. Solution in methyl acetate.
SOLUBILITY:
3mg/ml soluble in 100% ethanol, DMSO or dimethyl formamide; 0.5mg/ml soluble in a 1:1 solution of ethanol:PBS (pH 7.2) (dilute the ethanol solution with PBS).
SHIPPING:
SHIPPED ON DRY ICE
LONG TERM STORAGE:
-80°C
USE/STABILITY:
Stable for at least one year after receipt when stored at -80°C. We do not recommend storing aqueous solutions for more than one day.
Product Description
Selective, active-site directed, irreversible inhibitor of cPLA
2
and iPLA
2.
Potent inhibitor of fatty acid amide hydrolase (FAAH) (IC
50
=2.5nM), 800 -fold more potent than AACOCF
3
(Prod. No.
ALX-340-001
). Binds to the CB
1
receptor in rat brain membrane (IC
50
=20nM).
Product Specific Literature References
Methyl arachidonyl fluorophosphonate: a potent irreversible inhibitor of anandamide amidase:
D.G. Deutsch, et al.; Biochem. Pharmacol.
53
, 255 (1997)
Abstract
General Information
BACKGROUND/TECHNICAL INFORMATION
To change the solvent, evaporate the methyl acetate under a gentle stream of nitrogen and immediately add the solvent of choice.
Further Categories Containing This Product:
Cannabinoid Receptor Agonists & Antagonists / Related Products
•
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-340-041
Revised 11-Dec-07
Olvanil
SYNONYMS
NE-19550
N-Vanillyloleoylamide
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
TRPV1 Agonists and Antagonists / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-340-041-M005
5 mg
30.00 USD
ALX-340-041-M010
10 mg
48.00 USD
Product Specification
FORMULA:
C
26
H
43
NO
3
MW:
417.6
CAS NUMBER:
58493-49-5
PURITY:
≥98%
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in 100% ethanol, chloroform, dimethyl formamide or DMSO.
SHIPPING:
SHIPPED ON BLUE ICE
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
Product Description
"Hybrid" activator of CB
1
receptor (CB
1
: K
i
=1.6µM; CB
2
: K
i
=15µM) and TRPV1 (K
i
=0.4µM; EC
50
=33nM (human); EC
50
=6.71nM (rat)). Also inhibits anandamide uptake (IC
50
=9µM, K
i
=14.1µM) and fatty acid amide hydrolase (FAAH) (IC
50
=20µM).
Product Specific Literature References
NE-19550: a novel, orally active anti-inflammatory analgesic:
L. Brand, et al.; Drugs Exp. Clin. Res.
13
, 259 (1987)
Abstract
The antinociceptive effect and pharmacokinetics of olvanil following oral and subcutaneous dosing in the mouse:
W.K. Sietsema, et al.; Life Sci.
43
, 1385 (1988)
Abstract
Olvanil: more potent than capsaicin at stimulating the efferent function of sensory nerves:
S.R. Hughes, et al.; Eur. J. Pharmacol.
219
, 481 (1992)
Abstract
Interactions between synthetic vanilloids and the endogenous cannabinoid system:
V. Di Marzo, et al.; FEBS Lett.
436
, 449 (1998)
Abstract
Anandamide transport inhibition by the vanilloid agonist olvanil:
M. Beltramo & D. Piomelli; Eur. J. Pharmacol.
364
, 75 (1999)
Abstract
Unsaturated long-chain N-acyl-vanillyl-amides (N-AVAMs): vanilloid receptor ligands that inhibit anandamide-facilitated transport and bind to CB1 cannabinoid receptors:
D. Melck, et al.; BBRC
262
, 275 (1999)
Abstract
Vanilloid receptors on sensory nerves mediate the vasodilator action of anandamide:
P.M. Zygmunt, et al.; Nature
400
, 452 (1999)
Abstract
Overlap between the ligand recognition properties of the anandamide transporter and the VR1 vanilloid receptor: inhibitors of anandamide uptake with negligible capsaicin-like activity:
L. De Petrocellis, et al.; FEBS Lett.
483
, 52 (2000)
Abstract
Characterization using FLIPR of rat vanilloid receptor (rVR1) pharmacology:
J.C. Jerman, et al.; Br. J. Pharmacol.
130
, 916 (2000)
Abstract
Evidence against the presence of an anandamide transporter
:
S.T. Glaser, et al.; PNAS
100
, 4269 (2003)
Abstract
Identification of species-specific determinants of the action of the antagonist capsazepine and the agonist PPAHV on TRPV1
:
E. Phillips, et al.; J. Biol. Chem.
279
, 17165 (2004)
Abstract
Effects of the vanilloid agonist olvanil and antagonist capsazepine on rat behaviors:
J.W. Kasckow, et al.; Prog. Neuropsychopharmacol. Biol. Psychiatry
28
, 291 (2004)
Abstract
Further Categories Containing This Product:
Anandamide Uptake Inhibitors
•
Cannabinoid Receptor Agonists & Antagonists / Related Products
•
Fatty Acid Amide Hydrolase [FAAH] / Related Products
ALX-300-146
Revised 20-Jun-08
Palmitoylethanolamide
SYNONYMS
PEA
PRODUCT LINE
Neurobiology
