BQ-123

Pricing Availability Delivery Time Qty
Cat.No. 1188 - BQ-123 | cyclo(D-Trp-D-Asp-Pro-D-Val-Leu) | CAS No. 136553-81-6
Description: Selective ETA antagonist
Datasheet
Citations (3)
Literature

Biological Activity

Selective ETA endothelin receptor antagonist (Ki values are 1.4 and 1500 nM at ETA and ETB receptors respectively). Reduces ischemia-induced ventricular arrhythmias in a rat model.

Technical Data

M. Wt 611
Formula C31H42N6O7
Sequence WDPVL

(Modifications: Trp-1 = D-Trp, Val-4 = D-Val, Cyclized)

Storage Desiccate at -20°C
CAS Number 136553-81-6
PubChem ID 52943236
InChI Key VYCMAAOURFJIHD-AOYLRGCGSA-N
Smiles CC(C)C[C@@H]1NC(=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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 0.40 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 611. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.64 mL 8.18 mL 16.37 mL
5 mM 0.33 mL 1.64 mL 3.27 mL
10 mM 0.16 mL 0.82 mL 1.64 mL
50 mM 0.03 mL 0.16 mL 0.33 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Agapitov and Haynes (2002) Role of endothelin in cardiovascular disease. J.Renin Angiotensin Aldosterone Syst. 3 1 PMID: 11984741

Ekelund et al (1994) Effects of selective ETB-receptor stimulation on arterial, venous and capillary functions in cat skeletal muscle. Br.J.Pharmacol. 112 887 PMID: 7921617

Makatani et al (2000) Effect of a novel bifunctional endothelin receptor antagonist, IRL 3630A, on guinea pig respiratory mechanics. Eur.J.Pharmacol. 406 139 PMID: 11011045

Sakamoto et al (1993) Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J.Biol.Chem. 268 8547 PMID: 8473300


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Keywords: Selective ETA antagonists Receptors Endothelin Endothelin ETA Receptors

3 Citations for BQ-123

Citations are publications that use Tocris products. Selected citations for BQ-123 include:

Faraco et al (2014) Water deprivation induces neurovascular and cognitive dysfunction through vasopressin-induced oxidative stress. Am J Pathol 34 852 PMID: 24517977

Patel et al (2014) Activation of the endothelin system mediates pathological angiogenesis during ischemic retinopathy. J Neurosci 184 3040 PMID: 25203536

McQueen et al (2007) Endothelin-1 activates ETA receptors to cause reflex scratching in BALB/c mice. Br J Pharmacol 151 278 PMID: 17351652


Do you know of a great paper that uses BQ-123 from Tocris? If so please let us know.

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Literature in this Area

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Pathways for BQ-123

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