BQ788

Product details

• Chemical name: (2R)-2-[[(2R)-2-[[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]-3-(1-methoxycarbonylindol-3-yl)propanoyl]amino]hexanoic acid.
• CAS number: 173326-37-9
• Molecular formula: C34H51N5O7.
• Purity: >95%
• Concentration: 10-100 nM.
• Form: Lyophilized Powder
• Solubility: Soluble in DMSO and ethanol. 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-B receptor
• Source: Synthetic
• Activity: BQ788 is a potent and highly specific ET-B receptor antagonist, exhibiting selectivity for ET-B over ET-A human receptors when inhibiting the binding of [125I]-Endothelin-1 (IC50 of 1.2 nM and 1300 nM, respectively)1.

Scientific background

BQ788 is a synthetic modified tripeptide that acts as a potent, selective and competitive antagonist of the ET-B (endothelin B) receptor, a receptor that belongs to the G-protein coupled receptor (GPCR) superfamily. BQ788 is a soluble compound that does not bind plasma proteins and is metabolized in a short period of time. It lacks oral bioavailability and requires intra-arterial administration. The compound is used in vitro and in vivo to demonstrate the role of endogenous and exogenous endothelin receptor subtypes in physiological and pathophysiological conditions1,2. It displays IC50 values of 1.2 nM in radiolabeled Girardi heart cells and 1300 nM in human neuroblastoma cell line, respectively1.ET-A and ET-B receptors are widely distributed in vascular tissues where they mediate vasoconstriction and in nonvascular tissues such as the liver, kidney, and brain. ET-A receptors have high affinity for ET-1 and ET-2 peptides and relatively low affinity for ET-3, while ET-B receptors show high affinity for all ET isopeptides1.

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.

Bioassay tested: Yes

• SDS (PDF)

Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.

• Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
• Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
• Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
• QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
• Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity

To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).

Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).