BQ-123 sodium salt

BQ-123 sodium salt

Cyclo(D-trp-D-asp-L-pro-D-val-L-leu) sodium
A Selective Antagonist of Endothelin A Receptors
Cat #: B-185
Sizes: 5 mg, 10 mg, 25 mg, 50 mg
Source: Synthetic
MW: 632.69 Da.
Target: ET-A receptors
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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 an IC₅₀ value 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.

Endothelin receptors include two subtypes: 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 tissues to mediate vasoconstriction. They are also detected in several regions of the brain. ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while ET-B receptor has equally high affinity for all endothelin isopeptides³.

Alomone Labs is pleased to offer BQ-123 sodium salt (#B-185).

References

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

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Our bioassay

Alomone Labs BQ-123 sodium salt inhibits ETA 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™.
Purity>98%.
Effective concentration10 nM – 10 µM.
SequenceCyclo (D-trp-D-asp-L-pro-D-val-L-leu).
ModificationsSupplied as sodium salt.
Chemical name2-[(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 formulaC₃₁H₄₁N₆NaO₇.
CAS number136655-57-7.
ActivityBQ-123, a cyclic peptide provided here 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.
Storage before reconstitutionProduct before reconstitution should be stored desiccated at -20^oC.
ReconstitutionSoluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Storage after reconstitutionUp to three months at -20°C.