IRL 2500
Based on 1 Customer Validation
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.27%
- CAS. Nr.: 169545-27-1
- Formel: C36H35N3O4
- Molecular Weight:573.68
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Biologische Aktivität
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ETB 1.3 nM (IC50) |
ETA 94 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1.3 nM
Compound: 21; 1RL2500
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Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs
Displacement of [125I]ET-1 from human ET-B receptor expressed in CHO cell membrane incubated for 2 hrs
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[PMID: 27266371] |
| CHO | IC50 |
94 nM
Compound: 21; 1RL2500
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Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs
Displacement of [125I]ET-1 from human ET-A receptor expressed in CHO cell membrane incubated for 2 hrs
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[PMID: 27266371] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 169545-27-1
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Appearance Solid
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Molecular Weight 573.68
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Formel C36H35N3O4
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Color White to light yellow
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SMILES
O=C(O)[C@H](CC1=CNC2=CC=CC=C12)NC([C@@H](CC3=CC=C(C4=CC=CC=C4)C=C3)N(C(C5=CC(C)=CC(C)=C5)=O)C)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (174.31 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). 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). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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
Reinheit & Dokumentation
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Data Sheet (277 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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Handling Instructions (2659 KB)
Verweise
[1]. Balwierczak JL, et al. Characterization of a potent and selective endothelin-B receptor antagonist, IRL 2500.J Cardiovasc Pharmacol. 1995;26 Suppl 3:S393-6. [Content Brief]
[2]. Webb RL, et al. Effects of the ETB-selective antagonist IRL 2500 in conscious spontaneously hypertensive and Wistar-Kyoto rats.J Cardiovasc Pharmacol. 1995;26 Suppl 3:S389-92. [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). 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 | 1.7431 mL | 8.7157 mL | 17.4313 mL | 43.5783 mL |
| 5 mM | 0.3486 mL | 1.7431 mL | 3.4863 mL | 8.7157 mL | |
| 10 mM | 0.1743 mL | 0.8716 mL | 1.7431 mL | 4.3578 mL | |
| 15 mM | 0.1162 mL | 0.5810 mL | 1.1621 mL | 2.9052 mL | |
| 20 mM | 0.0872 mL | 0.4358 mL | 0.8716 mL | 2.1789 mL | |
| 25 mM | 0.0697 mL | 0.3486 mL | 0.6973 mL | 1.7431 mL | |
| 30 mM | 0.0581 mL | 0.2905 mL | 0.5810 mL | 1.4526 mL | |
| 40 mM | 0.0436 mL | 0.2179 mL | 0.4358 mL | 1.0895 mL | |
| 50 mM | 0.0349 mL | 0.1743 mL | 0.3486 mL | 0.8716 mL | |
| 60 mM | 0.0291 mL | 0.1453 mL | 0.2905 mL | 0.7263 mL | |
| 80 mM | 0.0218 mL | 0.1089 mL | 0.2179 mL | 0.5447 mL | |
| 100 mM | 0.0174 mL | 0.0872 mL | 0.1743 mL | 0.4358 mL |
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