BQ-123 trifluoroacetate

Product details

• 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] trifluoroacetate.
• Also known as: Cyclo(D-trp-D-asp-L-pro-D-val-L-leu) trifluoroacetate
• CAS number: 136553-81-6
• Molecular formula: C33H43F3N6O9.
• Purity: >98%
• Concentration: 10 nM - 10 µM.
• Form: Lyophilized powder.
• Solubility: Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
• Reconstitution: Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) 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. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (50 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: ET-A receptors
• Source: Synthetic
• Activity: BQ-123, a cyclic peptide, 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 KB of 40 nM1.
• Alternative names: Cyclo(D-trp-D-asp-L-pro-D-val-L-leu) trifluoroacetate

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 defense1,2.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.

Modifications

Supplied as trifluoroacetate salt.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Sequence

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

Bioassay tested: Yes

• SDS (PDF)

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