BMS 182874
Based on 1 Customer Validation
BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 153042-42-3
- Formula: C17H19N3O3S
- Molecular Weight:345.42
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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ETA 0.15 μM (IC50) |
ETA 0.055 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A10 | IC50 |
0.15 μM
Compound: 11
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Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
Ability to inhibit [125I]ET1 binding to vascular smooth muscle (vsm)- A10 cells
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[PMID: 8308857] |
| A10 | IC50 |
570 nM
Compound: 11
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Antagonism of ET-1 induced increase in intracellular Ca+2 in vsm-A10 cells
Antagonism of ET-1 induced increase in intracellular Ca+2 in vsm-A10 cells
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[PMID: 8308857] |
BMS-182874 (dimethyla minoanalogue 11) is an antagonist of the ETA ,with IC50 value of 0.150 μM and Ki of 0.055 μM in vsm-A10 cells, and with a KB value of 0.520 μM in rabbit carotid artery rings[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.
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Animal Model:Kidney Deoxycorticosterone acetate -salt hypertensive rats[1]
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Dosage:100 μM/kg
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Administration:Oral gavage (p.o.); Intravenous injection (i.v.)
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Result:Made arterial pressure slowly fell by 25% from a control level. After dosing for 12 and 24 h, makes arterial pressure is still 12% below the control level.
Chemical Information
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CAS No. 153042-42-3
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Appearance Solid
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Molecular Weight 345.42
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Formula C17H19N3O3S
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Color Light yellow to yellow
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SMILES
O=S(C1=C2C=CC=C(C2=CC=C1)N(C)C)(NC3=C(C(C)=NO3)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 125 mg/mL (361.88 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 (protect from 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 (protect from light). 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)
Purity & Documentation
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Data Sheet (276 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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 (protect from 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 | 2.8950 mL | 14.4751 mL | 28.9503 mL | 72.3757 mL |
| 5 mM | 0.5790 mL | 2.8950 mL | 5.7901 mL | 14.4751 mL | |
| 10 mM | 0.2895 mL | 1.4475 mL | 2.8950 mL | 7.2376 mL | |
| 15 mM | 0.1930 mL | 0.9650 mL | 1.9300 mL | 4.8250 mL | |
| 20 mM | 0.1448 mL | 0.7238 mL | 1.4475 mL | 3.6188 mL | |
| 25 mM | 0.1158 mL | 0.5790 mL | 1.1580 mL | 2.8950 mL | |
| 30 mM | 0.0965 mL | 0.4825 mL | 0.9650 mL | 2.4125 mL | |
| 40 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8094 mL | |
| 50 mM | 0.0579 mL | 0.2895 mL | 0.5790 mL | 1.4475 mL | |
| 60 mM | 0.0483 mL | 0.2413 mL | 0.4825 mL | 1.2063 mL | |
| 80 mM | 0.0362 mL | 0.1809 mL | 0.3619 mL | 0.9047 mL | |
| 100 mM | 0.0290 mL | 0.1448 mL | 0.2895 mL | 0.7238 mL |
BMS 182874 Related Classifications
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