BQ-788 (sodium salt)
Based on 14 publication(s) in Google Scholar
BQ-788 sodium salt is a potent and selective ETB receptor antagonist, inhibiting ET-1 binding to ETB receptors with an IC50 of 1.2 nM in human Girrardi heart cells.
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- 純度: 99.33%
- CAS 番号: 156161-89-6
- 分子式: C34H50N5NaO7
- 分子量:663.78
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保管条件:
-20°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 BQ-788 sodium salt
More- J Exp Clin Cancer Res. 2025 Feb 21;44(1):64. [Abstract]
- Cell Death Dis. 2026 Jan 16;17(1):45. [Abstract]
- J Orthop Translat. 2026 Feb 18:57:101048. [Abstract]
- Environ Pollut. 2016 Nov:218:487-496. [Abstract]
- Environ Pollut. 2016 Feb:209:11-20. [Abstract]
- Neurotherapeutics. 2021 Oct;18(4):2664-2681. [Abstract]
- Brain Pathol. 2026 Jan 14:e70067. [Abstract]
- Biochem Pharmacol. 2026 Aug;250(Pt 2):118027. [Abstract]
- Cells. 2021 Nov 8;10(11):3072. [Abstract]
- PLoS Pathog. 2020 Oct 19;16(10):e1008947. [Abstract]
- Toxicol Sci. 2016 Jan;149(1):213-26. [Abstract]
- J Neuroimmune Pharmacol. 2024 Apr 13;19(1):13. [Abstract]
- BMC Cancer. 2018 Feb 6;18(1):154. [Abstract]
- Environ Sci Pollut Res Int. 2018 May;25(15):14713-14725. [Abstract]
生物活性
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ETB |
BQ-788 potently and competitively inhibits 125I-labeled ET-1 binding to ETB receptors in human Girrardi heart cells with an IC50 of 1.2 nM, but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788 shows no agonistic activity up to 10 μM and competitively inhibits thevasoconstriction induced by an ETB-selective agonist (pA2, 8.4). BQ-788 also inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 156161-89-6
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性状 Solid
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分子量 663.78
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分子式 C34H50N5NaO7
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Color White to off-white
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SMILES
CCCC[C@H](C(O[Na])=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
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* The compound is unstable in solutions, freshly prepared is recommended.
Publications (14)
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Journal Impact Factor
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Most Recent
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J Exp Clin Cancer Res
The extracellular matrix protein type I collagen and fibronectin are regulated by β-arrestin-1/endothelin axis in human ovarian fibroblasts. [Abstract]2025 Feb 21;44(1):64. PMID: 39985042 -
Cell Death Dis
Nuclear gasdermin E drives endothelin-1-induced metastatic progression independently of the pyroptosis. [Abstract]2026 Jan 16;17(1):45. PMID: 41545335 -
J Orthop Translat
Endothelin-1/endothelin B receptor signalling mediates Prx1+ skeletal stem cells senescence: A driver of osteoporotic bone loss. [Abstract]2026 Feb 18:57:101048. PMID: 41757294 -
Environ Pollut
Airborne fine particulate matter alters the expression of endothelin receptors in rat coronary arteries. [Abstract]2016 Nov:218:487-496. PMID: 27461751 -
Environ Pollut
Airborne fine particulate matter induces an upregulation of endothelin receptors on rat bronchi. [Abstract]2016 Feb:209:11-20. PMID: 26618262 -
Neurotherapeutics
Crosstalk Among NLRP3 Inflammasome, ETBR Signaling, and miRNAs in Stress-Induced Depression-Like Behavior: a Modulatory Role for SGLT2 Inhibitors. [Abstract]2021 Oct;18(4):2664-2681. PMID: 34664178 -
Brain Pathol
Endothelial Netrin-4 regulates oligodendrocyte precursor cell proliferation and differentiation via ET-1 signaling in preterm white matter injury. [Abstract]2026 Jan 14:e70067. PMID: 41536029 -
Biochem Pharmacol
Bosentan confers cardioprotection against cisplatin toxicity: Involvement of β-arrestin-linked ETA receptor signaling. [Abstract]2026 Aug;250(Pt 2):118027. PMID: 42069228 -
Cells
2021 Nov 8;10(11):3072. PMID: 34831300 -
PLoS Pathog
Endothelin receptors promote schistosomiasis-induced hepatic fibrosis via splenic B cells. [Abstract]2020 Oct 19;16(10):e1008947. PMID: 33075079 -
Toxicol Sci
The Role of MAPK Pathways in Airborne Fine Particulate Matter-Induced Upregulation of Endothelin Receptors in Rat Basilar Arteries. [Abstract]2016 Jan;149(1):213-26. PMID: 26496744 -
J Neuroimmune Pharmacol
Endothelin-1-mediated Brainstem Glial Activation Produces Asthmatic Airway Vagal Hypertonia Via Enhanced ATP-P2X4 Receptor Signaling in Sprague-Dawley Rats. [Abstract]2024 Apr 13;19(1):13. PMID: 38613591 -
BMC Cancer
Overexpression of endothelin B receptor in glioblastoma: a prognostic marker and therapeutic target?. [Abstract]2018 Feb 6;18(1):154. PMID: 29409474 -
Environ Sci Pollut Res Int
Up-regulation of contractile endothelin receptors by airborne fine particulate matter in rat mesenteric arteries via activation of MAPK pathway. [Abstract]2018 May;25(15):14713-14725. PMID: 29536419
溶剤 & 溶解度
H2O : 50 mg/mL (75.33 mM; ultrasonic and warming and heat to 60°C)
DMSO : 25 mg/mL (37.66 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.77 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Okada M, et al. BQ-788, a selective endothelin ET(B) receptor antagonist. Cardiovasc Drug Rev. 2002 Winter;20(1):53-66. [Content Brief]
[2]. Sargent CA, et al. Effect of endothelin antagonists with or without BQ 788 on ET-1 responses in pithed rats. J Cardiovasc Pharmacol. 1995;26 Suppl 3:S216-8. [Content Brief]
[3]. Fattori V, et al. Differential regulation of oxidative stress and cytokine production by endothelin ETA and ETB receptors in superoxide anion-induced inflammation and pain in mice. J Drug Target. 2016 Oct 5:1-27 [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 1.5065 mL | 7.5326 mL | 15.0652 mL | 37.6631 mL |
| 5 mM | 0.3013 mL | 1.5065 mL | 3.0130 mL | 7.5326 mL | |
| 10 mM | 0.1507 mL | 0.7533 mL | 1.5065 mL | 3.7663 mL | |
| 15 mM | 0.1004 mL | 0.5022 mL | 1.0043 mL | 2.5109 mL | |
| 20 mM | 0.0753 mL | 0.3766 mL | 0.7533 mL | 1.8832 mL | |
| 25 mM | 0.0603 mL | 0.3013 mL | 0.6026 mL | 1.5065 mL | |
| 30 mM | 0.0502 mL | 0.2511 mL | 0.5022 mL | 1.2554 mL | |
| H2O | 40 mM | 0.0377 mL | 0.1883 mL | 0.3766 mL | 0.9416 mL |
| 50 mM | 0.0301 mL | 0.1507 mL | 0.3013 mL | 0.7533 mL | |
| 60 mM | 0.0251 mL | 0.1255 mL | 0.2511 mL | 0.6277 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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