BQ-123
Based on 4 publication(s) in Google Scholar
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension.
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- 純度: 99.91%
- CAS 番号: 136553-81-6
- 分子式: C31H42N6O7
- 分子量:610.70
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保管条件:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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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-123
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生物活性
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ETA |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A10 | IC50 |
14 nM
Compound: 1
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In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
In vitro inhibition of [125I]ET1 binding to rat A10 cell Endothelin A receptor.
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[PMID: 9667964] |
| CHO | IC50 |
20.5 nM
Compound: BQ-123
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Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
Displacement of [I125]ET1 from recombinant ETA receptor expressed in CHO cells after 2 hrs by TopCount analysis
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[PMID: 22862294] |
| CHO | IC50 |
>1000 nM
Compound: BQ-123
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Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
Displacement of [I125]ET1 from recombinant ETB receptor expressed in CHO cells after 2 hrs by TopCount analysis
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[PMID: 22862294] |
| SK-N-MC | IC50 |
0.62 nM
Compound: BQ-123
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Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method
Antagonist activity at ETA receptor in human SKNMC cells assessed as inhibition of endothelin-1-mediated Ca2+ mobilization by fura-2/AM dye-based spectrofluorimetric method
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[PMID: 27318985] |
BQ-123 (3 mg/kg; i.v.; given 15 minutes before pentylenetetrazole (PTZ)) impedes the formation and spread of seizure to a great degree in PTZ (50 mg/kg; i.p.) +BQ-123 groups[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar albino rats[5]
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Dosage:3 mg/kg
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Administration:Intravenous injection; given 15 minutes before PTZ
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Result:Number of rats with major seizure decreased.
化学情報
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CAS 番号 136553-81-6
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性状 Solid
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分子量 610.70
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分子式 C31H42N6O7
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Color White to off-white
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配列
Cyclo(d-Asp-Pro-d-Val-Leu-d-Trp)
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シーケンスの短縮
Cyclo(d-DP-d-VL-d-W)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (4)
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Journal Impact Factor
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Most Recent
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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 -
PLoS Pathog
Endothelin receptors promote schistosomiasis-induced hepatic fibrosis via splenic B cells. [Abstract]2020 Oct 19;16(10):e1008947. PMID: 33075079 -
Int Immunopharmacol
E. Coli LPS-induced calcium signaling regulates the expression of hypoxia-inducible factor 1α in periodontal ligament fibroblasts in a non-hypoxia-dependent manner. [Abstract]2024 Feb 15:128:111418. PMID: 38176341
溶剤 & 溶解度
DMSO : 50 mg/mL (81.87 mM; Need ultrasonic; 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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 5 mg/mL (8.19 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (8.19 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Ihara M, et al. In vitro biological profile of a highly potent novel endothelin (ET) antagonist BQ-123 selective for the ETA receptor. J Cardiovasc Pharmacol. 1992;20 Suppl 12:S11-S14. [Content Brief]
[2]. Sakamoto A, et al. Distinct subdomains of human endothelin receptors determine their selectivity to endothelinA-selective antagonist and endothelinB-selective agonists. J Biol Chem. 1993 Apr 25;268(12):8547-53. [Content Brief]
[3]. Zamora MA, et al. BQ123, an ETA receptor antagonist, inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells. Am J Respir Cell Mol Biol. 1993;9(4):429-433. [Content Brief]
[4]. Douglas SA, et al. BQ-123, a selective endothelin subtype A-receptor antagonist, lowers blood pressure in different rat models of hypertension. J Hypertens. 1994;12(5):561-567. [Content Brief]
[5]. Erdogan H et al. The protective effects of endothelin-A receptor antagonist BQ-123 in pentylenetetrazole-induced seizure in rats. Hum Exp Toxicol, 2014 Oct, 33(10):1008-16. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6375 mL | 8.1873 mL | 16.3747 mL | 40.9366 mL |
| 5 mM | 0.3275 mL | 1.6375 mL | 3.2749 mL | 8.1873 mL | |
| 10 mM | 0.1637 mL | 0.8187 mL | 1.6375 mL | 4.0937 mL | |
| 15 mM | 0.1092 mL | 0.5458 mL | 1.0916 mL | 2.7291 mL | |
| 20 mM | 0.0819 mL | 0.4094 mL | 0.8187 mL | 2.0468 mL | |
| 25 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6375 mL | |
| 30 mM | 0.0546 mL | 0.2729 mL | 0.5458 mL | 1.3646 mL | |
| 40 mM | 0.0409 mL | 0.2047 mL | 0.4094 mL | 1.0234 mL | |
| 50 mM | 0.0327 mL | 0.1637 mL | 0.3275 mL | 0.8187 mL | |
| 60 mM | 0.0273 mL | 0.1365 mL | 0.2729 mL | 0.6823 mL | |
| 80 mM | 0.0205 mL | 0.1023 mL | 0.2047 mL | 0.5117 mL |
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