Name: BQ-123 sodium salt
Brand: Alomone Labs
SKU: B-185

Cat #: B-185

Alternative Name Cyclo(D-trp-D-asp-L-pro-D-val-L-leu) sodium

Lyophilized Powder yes

Bioassay Tested

Source Synthetic

MW: 632.69

Purity: >98%

Effective concentration 10 nM – 10 µM.

Sequence Cyclo (D-trp-D-asp-L-pro-D-val-L-leu).

Modifications Supplied as sodium salt.

Structure

Chemical name 2-[(3R,6R,9S,12R,15S)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-3-yl] acetate sodium.

Molecular formula C₃₁H₄₁N₆NaO₇.

CAS No.: 136655-57-7

PubChem CID 443289

Activity BQ-123, a cyclic peptide provided as a sodium salt, is a potent and selective antagonist of ET-A endothelin receptors, exhibiting a 1000-fold selectivity for ET-A over ET-B receptors (inhibiting endothelin-1 radioligand binding to ET-A and ET-B with IC₅₀ of 22 nM and 18 µM, respectively). In vitro, BQ-123 inhibits endothelin-1 induced contractions of porcine coronary artery with K_B of 40 nM¹.

References-Activity

Moreland, S. (1994) Cardiovasc. Ther. 12, 48.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.

Solubility Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Storage of solutions Up to three months at -20°C.

Our bioassay

Alomone Labs BQ-123 sodium salt inhibits ET-A receptor-mediated Ca²⁺ mobilization in CHO cells.
Dose-response curve of BQ-123 sodium salt (#B-185) inhibition of the ET-A receptor-mediated, endothelin-1-evoked Ca²⁺ mobilization. Cells were loaded with Calcium 6 dye, incubated with BQ-123 sodium salt, and stimulated with 15 nM endothelin-1 (EC₈₀). Changes in intracellular Ca²⁺ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPR^TETRA™.

References - Scientific background

Moreland, S. (1994) Cardiovasc. Ther. 12, 48.
Kowalczyk, A. et al. (2016) Oxid. Med. Cell Longev. 2016, 2356853.
Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.

Scientific background

BQ-123 is a cyclic pentapeptide that acts as potent and selective antagonist of endothelin A (ET-A) receptors. BQ-123 exhibits a 1000-fold selectivity for ET-A receptors over ET-B receptors. It antagonizes endothelin-1 radioligand binding to ET-A and ET-B receptors with IC₅₀ values of 22 nM and 18 µM, respectively¹.

Studies show that BQ-123 prevents production of TNF-α and IL-6 in skeletal muscle of LPS-treated rat and enhances antioxidant defense^1,2.

There are two subtypes of endothelin receptor: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle where they mediate vasoconstriction. They are also detected in several regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides³.

Target ET-A receptors

Lyophilized Powder

Last update: 08/06/2022

BQ-123 sodium salt (#B-185) is a highly pure, synthetic, and biologically active compound.

Order Summary

BQ-123 sodium salt

Applications

Citations

Specifications

Scientific Background

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