A-192621
Based on 2 publication(s) in Google Scholar
A-192621, a chemical probe, is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
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- Pureza: 99.92%
- No. CAS: 195529-54-5
- Fòrmula: C33H38N2O6
- Peso molecular:558.66
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) A-192621
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Actividad biológica
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ETB 4.5 nM (IC50) |
ETB 8.8 nM (Ki) |
ETA 4280 nM (IC50) |
ETA 5600 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.65 nM
Compound: 38
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Antagonistic activity was measured by ET receptor mediated hydrolysis of inositol phosphates
Antagonistic activity was measured by ET receptor mediated hydrolysis of inositol phosphates
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[PMID: 10479298] |
A-192621 (1-100 μM; 48 hours; PASMCs) treatment markedly reduces the cell viability of PASMCs in a dose-dependent manner[2].
A-192621 (1-100 μM; 48 hours; PASMCs) treatment significantly increases the caspase-3/7 activity and cleaved caspase-3 expression in PASMCs. A-192621 induces apoptosis in a dose-dependent manner and increases the cells' susceptibility to apoptosis by Doxorubicin treatment[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
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Concentration:1 μM, 10 μM, 50 μM, 100 μM
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Incubation Time:72 hours
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Result:The viability of PASMCs was significantly decreased in a dose-dependent manner.
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Cell Line:Pulmonary arterial smooth muscle cells (PASMCs) with Doxorubicin
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Concentration:1 μM, 10 μM, 100 μM
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Incubation Time:72 hours
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Result:The caspase-3/7 activity in PASMCs was significantly increased in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (250-350 g)[3]
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Dosage:30 mg/kg 100 mg/kg
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Administration:Oral administration; daily; for 3 days
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Result:Inhibited both dilatory and pressor responses induced by S6c mediated by ETB with an ED50value of 30 mg/kg.
Chemical Information
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No. CAS 195529-54-5
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Appearance Solid
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Peso molecular 558.66
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Fòrmula C33H38N2O6
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Color White to off-white
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SMILES
O=C([C@H]1[C@H](C2=CC=C(OCCC)C=C2)N(CC(NC3=C(CC)C=CC=C3CC)=O)C[C@@H]1C4=CC=C(OCO5)C5=C4)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Function (Oxf)
High-Salt Diet Increases Suprachiasmatic Neuronal Excitability Through Endothelin Receptor Type B Signaling. [Abstract]2025 Mar 24;6(2):zqaf014. PMID: 40042980
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (179.00 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (4.47 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.
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.
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.
Pureza y Documentación
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Ficha de datos (284 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Wu-Wong JR, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: in vitro studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:107S-111S. [Content Brief]
[2]. Sakai S, et al. Antagonists to endothelin receptor type B promote apoptosis in human pulmonary arterial smooth muscle cells. Life Sci. 2016 Aug 15;159:116-120. [Content Brief]
[3]. Wessale JL, et al. Pharmacology of endothelin receptor antagonists ABT-627, ABT-546, A-182086 and A-192621: ex vivo and in vivo studies. Clin Sci (Lond). 2002 Aug;103 Suppl 48:112S-117S. [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. 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 | 1.7900 mL | 8.9500 mL | 17.9000 mL | 44.7499 mL |
| 5 mM | 0.3580 mL | 1.7900 mL | 3.5800 mL | 8.9500 mL | |
| 10 mM | 0.1790 mL | 0.8950 mL | 1.7900 mL | 4.4750 mL | |
| 15 mM | 0.1193 mL | 0.5967 mL | 1.1933 mL | 2.9833 mL | |
| 20 mM | 0.0895 mL | 0.4475 mL | 0.8950 mL | 2.2375 mL | |
| 25 mM | 0.0716 mL | 0.3580 mL | 0.7160 mL | 1.7900 mL | |
| 30 mM | 0.0597 mL | 0.2983 mL | 0.5967 mL | 1.4917 mL | |
| 40 mM | 0.0447 mL | 0.2237 mL | 0.4475 mL | 1.1187 mL | |
| 50 mM | 0.0358 mL | 0.1790 mL | 0.3580 mL | 0.8950 mL | |
| 60 mM | 0.0298 mL | 0.1492 mL | 0.2983 mL | 0.7458 mL | |
| 80 mM | 0.0224 mL | 0.1119 mL | 0.2237 mL | 0.5594 mL | |
| 100 mM | 0.0179 mL | 0.0895 mL | 0.1790 mL | 0.4475 mL |
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