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ALX-155-009
Revised 04-Feb-05
ETA-Receptor Antagonist [BE-18257B]
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-155-009-PC05
0.5 mg*
85.00 USD
ALX-155-009-P001
1 mg*
140.00 USD
Product Specification
SEQUENCE:
cyclo(D-Glu-Ala-allo-D-Ile-Leu-D-Trp)
FORMULA:
C
31
H
44
N
6
O
7
MW:
612.3
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥96%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Weak but highly selective ET
A
antagonist.
Product Specific Literature References
An endothelin receptor (ETA) antagonist isolated from Streptomyces misakiensis:
M. Ihara, et al.; BBRC
178
, 132 (1991)
Abstract
Endothelin-binding inhibitors, BE-18257A and BE-18257B. I. Taxonomy, fermentation, isolation and characterization:
K. Kojiri, et al.; J. Antibiot. (Tokyo)
44
, 1342 (1991)
Abstract
Endothelin-binding inhibitors, BE-18257A and BE-18257B II. Structure determination:
S. Nakajima, et al.; J. Antibiot. (Tokyo)
44
, 1348 (1991)
Abstract
WS-7338, new endothelin receptor antagonists isolated from Streptomyces sp. No. 7338. I. Taxonomy, fermentation, isolation, physico-chemical properties and biological activities:
S. Miyata, et al.; J. Antibiot. (Tokyo)
45
, 74 (1992)
Abstract
WS-7338, new endothelin receptor antagonists isolated from Streptomyces sp. No. 7338. III. Structures of WS-7338 A, B, C and D and total synthesis of WS-7338 B:
S. Miyata, et al.; J. Antibiot. (Tokyo)
45
, 788 (1992)
Abstract
Further Categories Containing This Product:
Peptides
ALX-155-004
Revised 11-Mar-05
ETA-Receptor Antagonist [BQ-123] . sodium salt
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-155-004-P001
1 mg*
95.00 USD
ALX-155-004-P005
5 mg*
380.00 USD
Product Specification
SEQUENCE:
cyclo(D-Asp-Pro-D-Val-Leu-D-Trp . Na)
FORMULA:
C
31
H
42
N
6
O
7
. Na
MW:
633.7
CAS NUMBER:
136553-81-6
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥96%
SOLUBILITY:
Soluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
USE/STABILITY:
Stable for at least 3 years after receipt when stored at -20°C. Stock solutions are stable for up to 3 months when stored at -20°C.
Product Description
Highly potent and selective ET
A
antagonist.
Product Specific Literature References
Identification of a domain of ETA receptor required for ligand binding
:
M. Adachi, et al.; FEBS Lett.
311
, 179 (1992)
Abstract
Conformational study of cyclo[D-Trp-D-Asp-Pro-D-Val-Leu], an endothelin- A receptor-selective antagonist:
R.A. Atkinson & J.T. Pelton; FEBS Lett.
296
, 1 (1992)
Abstract
A novel ETA antagonist (BQ-123) inhibits endothelin-1-induced phosphoinositide breakdown and DNA synthesis in rat vascular smooth muscle cells:
S. Eguchi, et al.; FEBS Lett.
302
, 243 (1992)
Abstract
Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor:
M. Ihara, et al.; Life Sci.
50
, 247 (1992)
Abstract
Cyclic pentapeptide endothelin antagonists with high ETA selectivity. Potency- and solubility-enhancing modifications:
K. Ishikawa, et al.; J. Med. Chem.
35
, 2139 (1992)
Abstract
Endothelin: progress in pharmacology and physiology:
W.G. Haynes, et al.; TIPS
14
, 225 (1993), (Review)
Abstract
Further Categories Containing This Product:
Peptides
ALX-155-011
Revised 04-Feb-05
ETA-Receptor Antagonist [BQ-610]
SYNONYMS
BQ-610
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-155-011-P001
1 mg*
125.00 USD
ALX-155-011-P005
5 mg*
500.00 USD
Product Specification
SEQUENCE:
(Hexahydro-1
H
-azepinyl)carbonyl-Leu-D-Trp(CHO)-D-Trp-OH
FORMULA:
C
36
H
44
N
6
O
6
MW:
656.8
QUANTITY:
*Sold as net peptide weight.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
30-fold more potent ET
A
antagonist than BQ-123 in pig aortic smooth muscle membrane assay, same activity as BQ-123 when tested on pig cerebellum membrane.
Further Categories Containing This Product:
Peptides
ALX-155-017
Revised 02-Dec-04
ETA-Receptor Antagonist [FR 139317]
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-155-017-PC05
0.5 mg*
180.00 USD
ALX-155-017-P001
1 mg*
340.00 USD
Product Specification
SEQUENCE:
(Hexahydro-1
H
-azepinyl)carbonyl-Leu-D-Trp(Me)-D-Ala(2-pyridyl)-OH
FORMULA:
C
32
H
43
N
6
O
5
MW:
605.8
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥97%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Selective ET
A
antagonist.
Product Specific Literature References
Structure-activity relationships of C-terminal endothelin hexapeptide antagonists:
A.M. Doherty, et al.; J. Med. Chem.
36
, 2585 (1993)
Abstract
Effect of different endothelin receptor antagonists and of the novel non-peptide antagonist Ro 46-2005 on endothelin levels in rat plasma:
B.-M. Löffler, et al.; FEBS Lett.
333
, 108 (1993)
Abstract
Further Categories Containing This Product:
Peptides
ALX-155-012
Revised 02-Dec-04
ETA-Receptor Antagonist [JKC-301]
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-155-012-PC05
0.5 mg*
85.00 USD
ALX-155-012-P001
1 mg*
140.00 USD
Product Specification
SEQUENCE:
cyclo(D-Asp-Pro-D-Ile-Leu-D-Trp)
FORMULA:
C
32
H
44
N
6
O
7
MW:
624.7
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥96%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Very potent ET
A
antagonist.
Product Specific Literature References
Lippton et al. ; American Heart Association, 66th Scientific Sessions, Georgia (World Congress, Nov. 8-11, 1993)
66
, 8 (1993)
The endothelin receptor profile in L6 myotubes:
Z. Fekete, et al.; Pharmacol. Exp. Ther.
275
, 215 (1995)
Abstract
Characterization of [125I]-endothelin-1 and [125I]-BQ3020 binding to rat cerebellar endothelin receptors:
P.S. Widdowson & C.N. Kirk; Br. J. Pharmacol.
118
, 2126 (1996)
Abstract
Further Categories Containing This Product:
Peptides
ALX-155-013
Revised 02-Dec-04
ETA-Receptor Antagonist [JKC-302]
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-155-013-PC05
0.5 mg*
85.00 USD
ALX-155-013-P001
1 mg*
140.00 USD
Product Specification
SEQUENCE:
cyclo(D-Ser-Pro-D-Val-Leu-D-Trp)
FORMULA:
C
30
H
42
N
6
O
6
MW:
582.7
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥96%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Very potent ET
A
antagonist.
Product Specific Literature References
Lippton et al.; American Heart Association, 66th Scientific Sessions, Georgia (World Congress, Nov. 8-11, 1993)
66
, 8 (1993)
Further Categories Containing This Product:
Peptides
ALX-155-020
Revised 17-Mar-08
ETB-Receptor Antagonist . sodium salt
SYNONYMS
BQ-788 . Na
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-155-020-MC05
0.5 mg
133.00 USD
ALX-155-020-M001
1 mg
185.00 USD
Product Specification
SEQUENCE:
N-
cis
-2,6-Dimethylpiperidinocarbonyl-L-γMeLeu-D-Trp(COOMe)-D-Nle-ONa
FORMULA:
C
34
H
50
N
5
O
7
Na
MW:
663.7
PEPTIDE CONTENT:
75-95%
PURITY:
≥95% (HPLC)
APPEARANCE:
White to off-white powder.
SOLUBILITY:
Soluble in methanol (0.5mg/ml), DMSO (4mg/ml), 0.1M sodium bicarbonate (3mg/ml) or 100% ethanol (4mg/ml); insoluble in water.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Highly potent and selective ET
B
-receptor antagonist.
Product Specific Literature References
Clearance of circulating endothelin-1 by ETB receptors in rats:
T. Fukuroda, et al.; BBRC
199
, 1461 (1994)
Abstract
Biochemical and pharmacological profile of a potent and selective endothelin B-receptor antagonist, BQ-788:
K. Ishikawa, et al.; PNAS
91
, 4892 (1994)
Abstract
Further Categories Containing This Product:
Peptides
ALX-155-010
Revised 05-Dec-04
ETB-Receptor Agonist [4 Ala ET-1]
SYNONYMS
[Ala
1,3,11,15
]-Endothelin-1
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-155-010-PC05
0.5 mg*
210.00 USD
ALX-155-010-P001
1 mg*
380.00 USD
Product Specification
SEQUENCE:
H-Ala-Ser-Ala-Ser-Ser-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp-OH
FORMULA:
C
109
H
163
N
25
O
32
MW:
2335.7
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥97%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Highly selective ligand for the ET
B
receptor.
Product Specific Literature References
[Ala1,3,11,15]endothelin-1 analogs with ETB agonistic activity:
T. Saeki, et al.; BBRC
179
, 286 (1991)
Abstract
Identification of high affinity endothelin-1 receptor subtypes in human tissues:
D.L. Williams Jrs., et al.; BBRC
180
, 475 (1991)
Abstract
Different distribution of endothelin receptor subtypes in pulmonary tissues revealed by the novel selective ligands BQ-123 and [Ala1,3,11,15]ET-1:
K. Nakamichi, et al.; BBRC
182
, 144 (1992)
Abstract
Solid-phase synthesis of [Ala1,3,11,15]-endothelin-1 by a modified double-coupling procedure:
J. Green; Int. J. Pept. Prot. Res.
41
, 492 (1993)
Abstract
Further Categories Containing This Product:
Peptides
ALX-155-015
Revised 02-Dec-04
ETB-Receptor Agonist [BQ-3020]
SYNONYMS
N-Acetyl-[Ala
11,15
]-Endothelin-1 (6-21)
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-155-015-PC05
0.5 mg*
90.00 USD
ALX-155-015-P001
1 mg*
160.00 USD
Product Specification
SEQUENCE:
Ac-Leu-Met-Asp-Lys-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp-OH
FORMULA:
C
96
H
140
N
20
O
25
S
MW:
2006.3
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥97%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Selective ligand for the ET
B
receptor.
Product Specific Literature References
A novel radioligand [125I]BQ-3020 selective for endothelin (ETB) receptors
:
M. Ihara, et al.; Life Sci.
51
, PL47 (1992)
Abstract
Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB- selective agonists:
A. Sakamoto, et al.; J. Biol. Chem.
268
, 8547 (1993)
Abstract
;
Full Text
Identification of a ligand-binding site of the human endothelin-A receptor and specific regions required for ligand selectivity:
M. Adachi, et al.; Eur. J. Biochem.
220
, 37 (1994)
Abstract
Further Categories Containing This Product:
Peptides
ALX-155-006
Revised 24-Feb-05
ETB-Receptor Agonist [IRL-1620]
SYNONYMS
Suc-[Glu
9
, Ala
11,15
]-Endothelin-1 (8-21)
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-155-006-PC05
0.5 mg*
100.00 USD
ALX-155-006-P001
1 mg*
175.00 USD
Product Specification
SEQUENCE:
Suc-Asp-Glu-Glu-Ala-Val-Tyr-Phe-Ala-His-Leu-Asp-Ile-Ile-Trp-OH
FORMULA:
C
86
H
117
N
17
O
27
MW:
1821.0
QUANTITY:
*Sold as net peptide weight.
PURITY:
≥97%
SHIPPING:
AMBIENT
LONG TERM STORAGE:
-20°C
Product Description
Most potent and selective ligand for the ET
B
receptor. IRL-1620 together with IRL-1038 (Prod. No.
ALX-155-007
) is an indispensable pharmacological tool to assess the participation of the ET
B
receptor in some pathophysiological phenomena, by selectively stimulating ET
B
receptor-mediated responses in various pathophysiological models established
in vitro
and
in vivo
.
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
Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB- selective agonists:
A. Sakamoto, et al.; J. Biol. Chem.
268
, 8547 (1993)
Abstract
;
Full Text
Endothelin: progress in pharmacology and physiology:
W.G. Haynes, et al.; TIPS
14
, 225 (1993), (Review)
Abstract
Further Categories Containing This Product:
Peptides
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:
Add To Cart
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
