BQ-3020

Aequorin functional assay / Calcium imaging assay

ET-B receptor

The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture.

2006 Da

A Selective and Potent Endothelin B Receptor Agonist

Centrifuge the vial (10, 000 × g for 5 minutes) before adding solvent to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Gently tap, tilt, and roll the vial to aid dissolution. Avoid vigorous vortexing; light vortexing for up to 3 seconds is acceptable if needed. Soluble in DMSO. Prepare a concentrated stock solution by dissolving the lyophilized peptide in DMSO first (e.g., at a concentration between 100-1000x of the final working concentration). Once the peptide is completely dissolved in DMSO, slowly dilute the solution into the working buffer (or water) to the desired final working concentration. Centrifuge all product preparations before use. Avoid multiple freeze-thaw cycles to maintain biological activity. It is recommended to keep the DMSO concentration as low as possible. For cell assays, a final concentration of 0.1%–0.5% DMSO (v/v) is considered safe. For other experiments, a 5% DMSO (v/v) concentration is recommended.

7, 4

Leu¹ = N-terminal Acetyl

BQ-3020 is a selective and potent ET-B receptor agonist1.

no

BQ-3020 is a synthetic peptide that acts as a selective and potent ET-B (endothelin B) receptor agonist, a receptor that belongs to the G protein-coupled receptors (GPCR). BQ-3020 is a linear analog of the ET-B receptor ligand endothelin 1 (ET-1), with very close structural similarity to ET-1 compared to other agonists. Several studies have shown that locally active in vivo administration of BQ-3020 causes arterial constriction in healthy human blood vessels1.Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-B receptor has high equal affinity for all endothelin isopeptides2. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia3.Endothelin receptor agonists are being used as useful tools for the functional characterization of these receptors. Studies have shown that administering ET-B receptor agonist into the rat renal medulla, leads to natriuresis and diuresis via a mechanism that is NOS1-dependent4.