Ro 46-8443
Based on 1 Customer Validation
Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM).
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: 98.93%
- CAS 番号: 175556-12-4
- 分子式: C31H35N3O8S
- 分子量:609.69
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保管条件:
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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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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ETB 34-69 nM (IC50) |
ETA 6800 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.069 μM
Compound: 19; Ro 46-8443
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Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
Antagonist activity at human ETB receptor expressed in CHO cells in presence of ET1
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[PMID: 27321813] |
| Sf9 | IC50 |
6.8 μM
Compound: 19; Ro 46-8443
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Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
Displacement of radioligand from ETA receptor (unknown origin) expressed in fall armyworm sf9 cell membranes
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[PMID: 27321813] |
化学情報
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CAS 番号 175556-12-4
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性状 Solid
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分子量 609.69
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分子式 C31H35N3O8S
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Color White to off-white
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SMILES
O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=NC(C3=CC=C(OC)C=C3)=NC(OC[C@H](O)CO)=C2OC4=CC=CC=C4OC)=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, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
DMSO : 250 mg/mL (410.04 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.
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: ≥ 2.08 mg/mL (3.41 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: 2.08 mg/mL (3.41 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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)
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 (277 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Breu V, et al. In vitro characterisation of Ro 46-8443, the first non-peptide antagonist selective for the endothelin ETB receptor. FEBS Lett. 1996;383(1-2):37-41. [Content Brief]
[2]. Clozel M, et al. The role of ETB receptors in normotensive and hypertensive rats as revealed by the non-peptide selective ETB receptor antagonist Ro 46-8443. FEBS Lett. 1996;383(1-2):42-45. [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 | 1.6402 mL | 8.2009 mL | 16.4018 mL | 41.0044 mL |
| 5 mM | 0.3280 mL | 1.6402 mL | 3.2804 mL | 8.2009 mL | |
| 10 mM | 0.1640 mL | 0.8201 mL | 1.6402 mL | 4.1004 mL | |
| 15 mM | 0.1093 mL | 0.5467 mL | 1.0935 mL | 2.7336 mL | |
| 20 mM | 0.0820 mL | 0.4100 mL | 0.8201 mL | 2.0502 mL | |
| 25 mM | 0.0656 mL | 0.3280 mL | 0.6561 mL | 1.6402 mL | |
| 30 mM | 0.0547 mL | 0.2734 mL | 0.5467 mL | 1.3668 mL | |
| 40 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0251 mL | |
| 50 mM | 0.0328 mL | 0.1640 mL | 0.3280 mL | 0.8201 mL | |
| 60 mM | 0.0273 mL | 0.1367 mL | 0.2734 mL | 0.6834 mL | |
| 80 mM | 0.0205 mL | 0.1025 mL | 0.2050 mL | 0.5126 mL | |
| 100 mM | 0.0164 mL | 0.0820 mL | 0.1640 mL | 0.4100 mL |
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