BQ-788 |
Catalog No.GC35546
One-Click Copy Product Info
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BQ-788 is a selective nonpeptide endothelin type B (ETB) receptor antagonist with an IC50 of 1.2nM. BQ-788 can specifically bind to ETB receptors, blocking the interaction between endothelin and its receptors, thereby inhibiting endothelin-mediated effects such as vasoconstriction and cell proliferation.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 173326-37-9
Sample solution is provided at 25 µL, 10mM.
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BQ-788 is a selective nonpeptide endothelin type B (ETB) receptor antagonist with an IC50 of 1.2nM[1]. BQ-788 can specifically bind to ETB receptors, blocking the interaction between endothelin and its receptors, thereby inhibiting endothelin-mediated effects such as vasoconstriction and cell proliferation[2]. BQ-788 is used to investigate the mechanisms of ETB in the cardiovascular system, including diseases like hypertension and heart failure[3]. BQ-788 can also be used to study the role of ETB in the nervous system, such as neuroprotection and neuroinflammation[4].
In vitro, BQ-788 (1μM) co-treated with fibrinogen (Fg; 4mg/mL) in rat heart microvascular endothelial cells (RHMECs) for 45 minutes significantly attenuated the phosphorylation of extracellular signal-regulated kinase 1/2 (ERK-1/2) induced by Fg[5]. BQ-788 (10μM) pre-treated rat olfactory mucosa cells for 1 week had no significant effect on cell proliferation but significantly increased the expression level of endogenous endothelin-1 (ET-1)[6].
In vivo, BQ-788 (0.2, 1, and 5mg/kg) was intravenously injected into ICR mice, followed by stimulation with ET-1 (0.1μmol/kg), and BQ-788 significantly inhibited ET-1-induced bronchoconstriction in mice[7]. BQ-788 (30nmol) co-injected subcutaneously with ET-1 (100pmol) into C57BL/6J mice significantly enhanced ET-1-induced scratching behavior[8].
References:
[1] Okada M, Nishikibe M. BQ-788, a selective endothelin ET(B) receptor antagonist. Cardiovasc Drug Rev. 2002 Winter;20(1):53-66.
[2] O'Donnell SR, Kay CS. Effects of endothelin receptor selective antagonists, BQ-123 and BQ-788, on IRL 1620 and endothelin-1 responses of airway and vascular preparations from rats. Pulm Pharmacol. 1995 Feb;8(1):11-9.
[3] Schroeder RL, Keiser JA, Cheng XM, et al. PD 142893, SB 209670, and BQ 788 selectively antagonize vascular endothelial versus vascular smooth muscle ET(B)-receptor activity in the rat. J Cardiovasc Pharmacol. 1998 Dec;32(6):935-43.
[4] Costa RA, Amatnecks JA, de Oliveira Guaita G, et al. Sexual dimorphism of hypothalamic serotonin release during systemic inflammation: Role of endothelin-1. J Neuroimmunol. 2024 Sep 15;394:578427.
[5] Sen U, Tyagi N, Patibandla PK, et al. Fibrinogen-induced endothelin-1 production from endothelial cells. Am J Physiol Cell Physiol. 2009 Apr;296(4):C840-7.
[6] Bryche B, Saint-Albin A, Le Poupon Schlegel C, et al. Endothelin increases the proliferation of rat olfactory mucosa cells. Neural Regen Res. 2020 Feb;15(2):352-360.
[7] Nagase T, Aoki T, Oka T, et al. ET-1-induced bronchoconstriction is mediated via ETB receptor in mice. J Appl Physiol (1985). 1997 Jul;83(1):46-51.
[8] Liang J, Kawamata T, Ji W. Molecular signaling of pruritus induced by endothelin-1 in mice. Exp Biol Med (Maywood). 2010 Nov;235(11):1300-5.
| Cell experiment [1]: | |
Cell lines | Rat heart microvascular endothelial cells (RHMECs) |
Preparation Method | RHMECs were grown in MCDB-131 complete medium at 37°C, 5% CO₂. Cells were serum-deprived for 1h using MCDB-131C medium without serum before experimentation. Cells were treated with 4mg/ml Fibrinogen (Fg) with or without 1μM BQ-788 for 45min. |
Reaction Conditions | 1μM; 45min |
Applications | BQ-788 significantly attenuated the Fg-induced phosphorylation of ERK-1/2 in RHMECs. |
| Animal experiment [2]: | |
Animal models | ICR mice |
Preparation Method | Mice were anesthetized and mechanically ventilated. They were pretreated with BQ-788 (0.2, 1, or 5mg/kg) via intravenous injection before administration of ET-1 (0.1μmol/kg) |
Dosage form | 0.2, 1, or 5mg/kg; i.v. |
Applications | BQ-788 significantly inhibited ET-1-induced bronchoconstriction, suggesting that ETB receptors mediate ET-1-induced airway narrowing by affecting airway smooth muscle contraction. |
References: | |
| Cas No. | 173326-37-9 | SDF | |
| Canonical SMILES | CCCC[C@H](C(O)=O)NC([C@@H](CC1=CN(C(OC)=O)C2=CC=CC=C12)NC([C@H](CC(C)(C)C)NC(N3[C@H](C)CCC[C@@H]3C)=O)=O)=O | ||
| Formula | C34H51N5O7 | M.Wt | 641.8 |
| Solubility | DMSO : 100 mg/mL (155.81 mM; Need ultrasonic) | Storage | Store at -20°C,protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.5581 mL | 7.7906 mL | 15.5812 mL |
| 5 mM | 311.6 μL | 1.5581 mL | 3.1162 mL |
| 10 mM | 155.8 μL | 779.1 μL | 1.5581 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 19 reference(s) in Google Scholar.)