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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.85%
- CAS 番号: 153042-42-3
- 分子式: C17H19N3O3S
- 分子量:345.42
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保管条件:
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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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
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生物活性
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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.
化学情報
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CAS 番号 153042-42-3
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性状 Solid
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分子量 345.42
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (393 KB)
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取扱説明書 (2659 KB)
参考文献
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 関連分類
HY-118497 関連分類
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