BQ-123 . sodium salt
| Code | Size | Price |
|---|
| AG-CP3-0001-M001 | 1 mg | £102.00 |
Quantity:
| AG-CP3-0001-M005 | 5 mg | £380.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
Ambient
Storage:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
Endothelin Receptor A Antagonist BQ-123; cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu) . Na
Appearance:
White solid.
CAS:
136655-57-7
EClass:
32160000
Form (Short):
liquid
Handling Advice:
After reconstitution, prepare aliquots and store at -20°C.
InChi:
InChI=1S/C31H42N6O7.Na/c1-16(2)12-21-27(40)33-22(13-18-15-32-20-9-6-5-8-19(18)20)28(41)35-23(14-25(38)39)31(44)37-11-7-10-24(37)29(42)36-26(17(3)4)30(43)34-21;/h5-6,8-9,15-17,21-24,26,32H,7,10-14H2,1-4H3,(H,33,40)(H,34,43)(H,35,41)(H,36,42)(H,38,39);/q;+1/p-1/t21-,22-,23-,24+,26-;/m1./s1
InChiKey:
FLIKEIGEOXCRRG-DRBUQPBJSA-M
Long Description:
Chemical. CAS: 136655-57-7. Formula: C31H42N6O7 . Na. MW: 609.7 . 23.0. Synthetic. Potent and selective endothelin receptor A (ETA) antagonist. Suppresses the ET-1-induced decrease of LPL activity. Shows protective effects in ischemic acute renal failure. Neuroprotective. Anti-hypertensive. Inhibits ET-1 receptor binding and blocks Ca2+ mobilization, cellular contraction and MAP kinase activation. Cardiovascular agent. Reduces myocardial infarct size and oxidant injury. Selected Reviews.
MDL:
MFCD00905129
Molecular Formula:
C31H42N6O7 . Na
Molecular Weight:
609.7 . 23.0
Other data:
Net peptide content (AAA): 73.1%
Package Type:
Vial
Product Description:
Potent and selective endothelin receptor A (ETA) antagonist [1-3]. Suppresses the ET-1-induced decrease of LPL activity [4]. Shows protective effects in ischemic acute renal failure [5]. Neuroprotective [6, 10]. Anti-hypertensive [7]. Inhibits ET-1 receptor binding and blocks Ca2+ mobilization, cellular contraction and MAP kinase activation [8]. Cardiovascular agent [9]. Reduces myocardial infarct size and oxidant injury [11]. Selected Reviews [12, 13].
Purity:
>98% (HPLC)
SMILES:
[Na+].CC(C)CC1NC(=O)[C@H](NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CC([O-])=O)NC(=O)[C@@H](CC2=CNC3=C2C=CC=C3)NC1=O)C(C)C
Solubility Chemicals:
Soluble in water.
Source / Host:
Synthetic.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 3 years after receipt when stored at -20°C.
References
In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor: M. Ihara, et al.; J. Cardiovasc. Pharmacol. 20, S11 (1992) | BQ-123, cyclo(-D-Trp-D-Asp-Pro-D-Val-Leu), is a non-competitive antagonist of the actions of endothelin-1 in SK-N-MC human neuroblastoma cells: C.R. Hiley, et al.; BBRC 184, 504 (1992) | Biological profiles of highly potent novel endothelin antagonists selective for the ETA receptor: M. Ihara, et al.; Life Sci. 50, 247 (1992) | Suppressive effects of the endothelin receptor (ETA) antagonist BQ-123 on ET-1-induced reduction of lipoprotein lipase activity in 3T3-L1 adipocytes: F. Ishida, et al.; Biochem. Pharmacol. 44, 1431 (1992) | Protective effect of a selective endothelin receptor antagonist, BQ-123, in ischemic acute renal failure in rats: N. Mino, et al.; Eur. J. Pharmacol. 221, 77 (1992) | Peptidic endothelin-1 receptor antagonist, BQ-123, and neuroprotection: G. Feuerstein, et al.; Peptides 15, 467 (1994) | BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension: S.A. Douglas, et al.; J. Hypertens. 12, 561 (1994) | Inhibitory effect of BQ-123 on endothelin-1-stimulated mitogen-activated protein kinase and cell growth of rat vascular smooth muscle cells: X. Guo, et al.; Hypertens. Res. 19, 23 (1996) | Inhibition of myocardial endothelin pathway improves longterm survival in heart failure: S. Sakai, et al.; Nature 384, 353 (1996) | Similar protective effects of BQ-123 and erythropoietin on survival of neural cells and generation of neurons upon hypoxic injury: L. Danielyan, et al.; Eur. J. Cell Biol. 84, 907 (2005) | Selective endothelin a (ETA) receptor antagonist (BQ-123) reduces both myocardial infarct size and oxidant injury: R. Ozdemir, et al.; Toxicology 219, 142 (2006) | Endothelin receptor antagonists: S. Motte, et al.; Pharmacol. Ther. 110, 386 (2006) (Review) | ETA-receptor antagonists or allosteric modulators?: J.G. De Mey, et al.; TIPS 32, 345 (2011) (Review)