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ALX-155-007
Revised 24-Feb-05
ETB-Receptor Antagonist [IRL-1038]
SYNONYMS
[Cys
11
-Cys
15
]-Endothelin-1 (11-21)
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Endothelins [ETs] & Endothelin Receptors / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
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ALX-155-007-PC05
0.5 mg*
110.00 USD
ALX-155-007-P001
1 mg*
190.00 USD
Product Specification
SEQUENCE:
H-Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trp-OH
(Disulfide bonds between Cys
1
-Cys
5
)
FORMULA:
C
68
H
92
N
14
O
15
S
2
MW:
1409.7
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥97%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Antagonist for the ET
B
receptor with a controversial pattern of activity.
Product Specific Literature References
A potent and specific agonist, Suc-[Glu9,Ala11,15]-endothelin-1(8-21), IRL 1620, for the ETB receptor:
M. Takai, et al.; BBRC
184
, 953 (1992)
Abstract
An endothelin B receptor-selective antagonist: IRL 1038, [Cys11-Cys15]- endothelin-1(11-21) [retracted in: FEBS Lett 1994 Mar 28;342(1):103]:
Y. Urade, et al.; FEBS Lett.
311
, 12 (1992)
Abstract
Endothelin: progress in pharmacology and physiology:
W.G. Haynes, et al.; TIPS
14
, 225 (1993), (Review)
Abstract
An endothelin B receptor-selective antagonist: IRL 1038, [Cys11- Cys15]- endothelin-1(11-21):
Y. Urade, et al.; FEBS Lett.
342
, 103 (1994)
Abstract
Further Categories Containing This Product:
Peptides
ALX-155-018
Revised 23-Oct-07
ETB-Receptor Antagonist [RES-701-1]
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Endothelins [ETs] & Endothelin Receptors / Related Products
Ordering Information
Product Numbers:
Format:
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ALX-155-018-MC05
0.5 mg
130.00 USD
ALX-155-018-M001
1 mg
200.00 USD
Product Specification
SEQUENCE:
Gly-Asn-Trp-His-Gly-Thr-Ala-Pro-Asp-Trp-Phe-Phe-Asn-Tyr-Tyr-Trp-OH
(Beta peptide bond between Gly
1
and Asp
9
).
FORMULA:
C
103
H
115
N
23
O
23
MW:
2043.2
PEPTIDE CONTENT:
75-90%
PURITY:
≥97% (HPLC)
FORMULATION:
Lyophilized.
SOLUBILITY:
Soluble in DMSO (5mg/ml); dilute with 0.6ml distilled water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Inhibits selectively the ET-1 binding to the ET
B
receptor.
Product Specific Literature References
RES-701-1, a novel and selective endothelin type B receptor antagonist produced by Streptomyces sp. RE-701. I. Characterization of producing strain, fermentation, isolation, physico-chemical and biological properties:
Y. Morishita, et al.; J. Antibiot.
47
, 269 (1994)
Abstract
Subtypes of endothelin ETA and ETB receptors mediating venous smooth muscle contraction:
S.A. Sudjarwo, et al.; BBRC
200
, 627 (1994)
Abstract
J.X. He, et al.; Bioorg. Med. Chem. Lett.
5
, 621 (1995)
Further Categories Containing This Product:
Peptides
ALX-155-019
Revised 02-Dec-04
ETB-Receptor Antagonist [RES-701-3]
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Endothelins [ETs] & Endothelin Receptors / Related Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-155-019-MC05
0.5 mg
130.00 USD
ALX-155-019-M001
1 mg
240.00 USD
Product Specification
SEQUENCE:
Gly-Asn-Trp-His-Gly-Thr-Ser-Pro-Asp-Trp-Phe-Phe-Asn-Tyr-Tyr-Trp-OH
(Beta peptide bond between Gly
1
and Asp
9
).
FORMULA:
C
103
H
115
N
23
O
24
MW:
2059.2
PURITY:
≥97%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Further Categories Containing This Product:
Peptides
ALX-550-324
Revised 28-Jan-05
(2S)-α-Ethylglutamic acid
SYNONYMS
EGLU
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Glutamate Receptors (Metabotropic) / Related Products
Ordering Information
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ALX-550-324-M001
1 mg
35.00 USD
ALX-550-324-M005
5 mg
95.00 USD
Product Specification
FORMULA:
C
7
H
13
NO
4
MW:
175.2
PURITY:
≥98%
APPEARANCE:
White solid.
SOLUBILITY:
Soluble in dilute aqueous base.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
Product Description
Group II mGluR antagonist.
Product Specific Literature References
Potent antagonists at the L-AP4- and (1S,3S)-ACPD-sensitive presynaptic metabotropic glutamate receptors in the neonatal rat spinal cord:
D.E. Jane, et al.; Neuropharmacology
35
, 1029 (1996)
Abstract
Group 1 and 2 metabotropic glutamate receptors play differential roles in hippocampal long-term depression and long-term potentiation in freely moving rats:
D. Manahan-Vaughan; J. Neurosci.
17
, 3303 (1997)
Abstract
Bidirectional synaptic plasticity in the rat basolateral amygdala: characterization of an activity-dependent switch sensitive to the presynaptic metabotropic glutamate receptor antagonist 2S-alpha-eth:
H. Li, et al.; J. Neurosci.
18
, 1662 (1998)
Abstract
Induction of long-lasting depression by (+)-alpha-methyl-4-carboxyphenylglycine and other group II mGlu receptor ligands in the dentate gyrus of the hippocampus in vitro:
L. Huang, et al.; Eur. J. Pharmacol.
366
, 151 (1999)
Abstract
Pharmacological agents acting at subtypes of metabotropic glutamate receptors
:
D.D. Schoepp, et al.; Neuropharmacology
38
, 1431 (1999), (Review)
Abstract
ALX-290-002
Revised 13-Dec-04
S-Farnesylated Cysteine Tetrapeptide
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
Ordering Information
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ALX-290-002-M001
1 mg
45.00 USD
ALX-290-002-M005
5 mg
150.00 USD
Product Specification
SEQUENCE:
Ac-Cys(farnesyl)-Val-Ile-Met-OH
FORMULA:
C
36
H
62
N
4
O
6
S
2
MW:
711.0
PURITY:
≥95%
APPEARANCE:
Yellow solid.
SOLUBILITY:
Soluble in chloroform.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Hygroscopic. Protect from light and oxygen.
Product Description
Tetrapeptide substrate for the protein endoprotease that cleaves the modified protein at the isoprenylated cysteine residue.
Product Specific Literature References
Inhibitors of the isoprenylated protein endoprotease:
Y.-T. Ma, et al.; Biochemistry
32
, 2386 (1993)
Abstract
ALX-290-003
Revised 30-Jun-08
Farnesylpyrophosphate . triammonium salt
SYNONYMS
FPP . 3NH
4
3,7,11-Trimethyl-2,6,10-dodecatrien-1-ol pyrophosphate . 3NH
4
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
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ALX-290-003-C200
200 µg
62.00 USD
Product Specification
FORMULA:
C
15
H
25
O
7
P
2
. 3NH
4
MW:
379.3 . 54.1
CAS NUMBER:
13058-04-3
PURITY:
≥98% (TLC)
APPEARANCE:
Liquid. Solution in 0.25M ammonium bicarbonate containing 70% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Store solutions at -20°C for up to 3 months.
HANDLING:
Protect from light and moisture.
Product Description
Farnesyl donor in enzymatic protein farnesylation catalyzed by farnesyltransferase.
Product Specific Literature References
Tautomycin from the bacterium Streptomyces verticillatus. Another potent and specific inhibitor of protein phosphatases 1 and 2A:
C. MacKintosh & S. Klumpp; FEBS Lett.
277
, 137 (1990)
Abstract
M. Ubukata, et al.; J. C. S. Chem. Commun. 244 (1990)
Divalent cation and prenyl pyrophosphate specificities of the protein farnesyltransferase from rat brain, a zinc metalloenzyme:
Y. Reiss, et al.; J. Biol. Chem.
267
, 6403 (1992)
Abstract
;
Full Text
Inhibitors of Ras farnesyltransferases:
F. Tamanoi; TIBS
18
, 349 (1993), (Review)
Abstract
Farnesyltransferase inhibitors: Ras research yields a potential cancer therapeutic:
J.B. Gibbs, et al.; Cell
77
, 175 (1994)
Abstract
ALX-290-004
Revised 25-Oct-06
Farnesylthioacetic acid
SYNONYMS
FTA
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
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ALX-290-004-M005
5 mg
90.00 USD
Product Specification
FORMULA:
C
17
H
28
O
2
S
MW:
296.5
CAS NUMBER:
135784-48-4
PURITY:
≥98%
APPEARANCE:
Yellow viscous oil.
SOLUBILITY:
Soluble in DMSO or 100% ethanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Solutions are stable for up to 6 months when stored at -20°C. Product is not sterile.
HANDLING:
Protect from light.
Product Description
Potent and specific inhibitor of methyl esterification of farnesylated proteins (e.g. the γ subunit of transducin). This compound is not a methyltransferase substrate.
Product Specific Literature References
Identifying the recognition unit for G protein methylation:
E.W. Tan, et al.; J. Biol. Chem.
266
, 10719 (1991)
Abstract
;
Full Text
ALX-290-005
Revised 10-Aug-05
Farnesyltransferase Inhibitor
SYNONYMS
B581
PRODUCT LINE
Signal Transduction
PRODUCT CATEGORY
Farnesylation / Isoprenylation Reagents
Ordering Information
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ALX-290-005-M001
1 mg
85.00 USD
ALX-290-005-M005
5 mg
320.00 USD
Product Specification
SEQUENCE:
N-[(2S)-((2R)-Amino-3-mercaptopropylamino)-3-methylbutyl]-Phe-Met-OH
FORMULA:
C
22
H
38
N
4
O
3
S
2
MW:
470.7
PURITY:
≥96%
APPEARANCE:
White powder.
SOLUBILITY:
Soluble in water or DMSO.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Hygroscopic.
Product Description
Stable, membrane permeable inhibitor of farnesyltransferase. Has 30-fold higher selectivity for farnesyltransferase over geranylgeranyltransferase. Potential anticancer drug.
Product Specific Literature References
Peptidomimetic inhibitors of Ras farnesylation and function in whole cells:
A.M. Garcia, et al.; J. Biol. Chem.
268
, 18415 (1993)
Abstract
;
Full Text
ALX-550-413
Revised 23-May-06
Fenobam
PRODUCT LINE
Neurobiology
PRODUCT CATEGORY
Glutamate Receptors (Metabotropic) / Related Products
Ordering Information
Product Numbers:
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ALX-550-413-M005
5 mg
60.00 USD
ALX-550-413-M025
25 mg
240.00 USD
Product Specification
FORMULA:
C
11
H
11
ClN
4
O
2
MW:
266.7
CAS NUMBER:
57653-26-6
PURITY:
≥98% (
1
H-NMR)
APPEARANCE:
Off-white to pale orange solid.
SOLUBILITY:
Soluble in DMSO or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
IDENTITY:
Determined by
1
H-NMR and
13
C-NMR.
Product Description
Potent and selective non-competitive mGluR5 antagonist that displays inverse agonist properties; blocks mGluR5 constitutive activity
in vitro
(IC
50
=87nM). Acts at an allosteric modulatory site shared with MPEP (Prod. No.
ALX-550-368
) and binds mGluR5 with Kd values of 54nM and 31nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration
in vivo
.
Product Specific Literature References
Novel non-benzodiazepine anxiolytics:
M.E. Goldberg, et al.; Neuropharmacology
22
, 1499 (1983)
Abstract
In vitro and in vivo metabolism of the antianxiolytic agent fenobam in the rat:
W.N. Wu, et al.; J. Pharm. Sci.
84
, 185 (1995)
Abstract
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity:
R.H. Porter, et al.; J. Pharmacol. Exp. Ther.
315
, 711 (2005)
Abstract
Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues:
A. Wallberg et al.; Bioorg. Med. Chem. Lett.
16
, 1142 (2006)
Abstract
Related Products
ALX-550-368
MPEP . hydrochloride
Further Categories Containing This Product:
Anxiolytic Agents / Related Products
ALX-380-052
Revised 16-Oct-07
Fusaric acid
SYNONYMS
5-Butylpicolinic acid
PRODUCT LINE
Natural Products / Antibiotics
PRODUCT CATEGORY
Antibiotics Other Products
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ALX-380-052-M050
50 mg
20.00 USD
Product Specification
FORMULA:
C
10
H
13
NO
2
MW:
179.2
CAS NUMBER:
536-69-6
MERCK INDEX:
14:
4314
SOURCE/HOST:
Isolated from
Gibberella fujikuroi
.
PURITY:
≥99%
APPEARANCE:
White solid.
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
HANDLING:
Protect from light.
HAZARD:
TOXIC.
Product Description
Antibiotic. Inhibitor of dopamine β-hydroxylase.
Product Specific Literature References
Biochemistry of the bakanaefungus. I. Fusarinic acid, a new product of the bakanae fungus:
T. Yubata, et al.; J. Agric. Chem. Soc. Jpn.
10
, 1059 (1934)
Pharmacological activities of fusaric acid (5-butylpicolinic acid):
H. Wang & T.B. Ng; Life Sci.
65
, 849 (1999), Review
Abstract
Further Categories Containing This Product:
Dopaminergics & Dopamine Receptors / Related Products
ALX-157-003
Revised 03-Mar-05
Galanin (human)
PRODUCT LINE
Obesity & Adipokines
PRODUCT CATEGORY
Galanin & Galanin Receptor / Related Products
Ordering Information
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ALX-157-003-PC05
0.5 mg*
190.00 USD
ALX-157-003-P001
1 mg*
280.00 USD
Product Specification
SEQUENCE:
H-Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-His-Ala-Val-Gly-Asn-His-Arg-Ser-Phe-Ser-Asp-Lys-Asn-Gly-Leu-Thr-Ser-OH
FORMULA:
C
139
H
210
N
42
O
43
MW:
3157.4
CAS NUMBER:
119418-04-1
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥98%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Specific Literature References
Galanin: profile of a new neuropeptide:
L.W. Haynes; TIPS
7
, 214 (1986), (Review)
Galanin - a newly isolated biologically active neuropeptide
:
A. Rökaeus; Trends Neurosci.
10
, 158 (1987)
Galanin and the endocrine pancreas:
B. Ahren, et al.; FEBS Lett.
229
, 233 (1988)
Abstract
Galanin. A selective inhibitor of insulin secretion?:
J. Dupré; Pancreas
3
, 119 (1988)
Abstract
Co-existence of galanin and acetylcholine: is galanin involved in memory processed and dementia?:
J.N. Crawley & G.L. Wenk; TINS
12
, 278 (1989)
Abstract
Inhibitory action of galanin on gastric acid secretion in pentobarbital-anesthetized rats:
W.J. Rossowski & D.H. Coy; Life Sci.
44
, 1807 (1989)
Abstract
Galanin in the porcine pancreas:
T. Messell, et al.; Regul. Pept.
28
, 161 (1990)