Talinolol
Based on 1 Customer Validation
Talinolol (Cordanum) is a long-acting, cardioselective β1-adrenergic receptor blocker. Talinolol exhibits cardioprotective and antihypertensive activities. Talinolol is also a well-known and frequently used probe substrate for P-glycoprotein (P-gp) activity.
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: 99.56%
- CAS 番号: 57460-41-0
- 分子式: C20H33N3O3
- 分子量:363.49
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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)
Adrenergic Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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Beta-1 adrenergic receptor |
Human OATP1A2-, rat Oatp1a5-, and rat Mdr1a-mediated Talinolol transport can be inhibited by naringin, with IC50s of 343, 12.7, and 604 μM, respectively, in LLC-PK1 cell and Xenopus laevis oocyte systems[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Bioavailability of Talinolol can be enhanced by coadministration with grapefruit juice (GFJ) in rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 57460-41-0
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性状 Solid
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分子量 363.49
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分子式 C20H33N3O3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(OCC(O)CNC(C)(C)C)C=C1)NC2CCCCC2
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別名
Talinolol; Cordanum
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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 : 100 mg/mL (275.11 mM; ultrasonic and warming and heat to 60°C; 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 (270 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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取扱説明書 (2659 KB)
参考文献
[1]. Assmann I. The actions of talinolol, a beta 1-selective beta blocker, in cardiac arrhythmia and acute myocardial infarction. Curr Med Res Opin. 1995;13(6):325-42. [Content Brief]
[2]. Kara ZP, et, al. The effects of P-glycoprotein inhibitor zosuquidar on the sex and time-dependent pharmacokinetics of parenterally administered talinolol in mice. Eur J Pharm Sci. 2021 Jan 1;156:105589. [Content Brief]
[3]. Shirasaka Y, et, al. Species difference in the effect of grapefruit juice on intestinal absorption of talinolol between human and rat. J Pharmacol Exp Ther. 2010 Jan;332(1):181-9. [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 (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 | 2.7511 mL | 13.7555 mL | 27.5111 mL | 68.7777 mL |
| 5 mM | 0.5502 mL | 2.7511 mL | 5.5022 mL | 13.7555 mL | |
| 10 mM | 0.2751 mL | 1.3756 mL | 2.7511 mL | 6.8778 mL | |
| 15 mM | 0.1834 mL | 0.9170 mL | 1.8341 mL | 4.5852 mL | |
| 20 mM | 0.1376 mL | 0.6878 mL | 1.3756 mL | 3.4389 mL | |
| 25 mM | 0.1100 mL | 0.5502 mL | 1.1004 mL | 2.7511 mL | |
| 30 mM | 0.0917 mL | 0.4585 mL | 0.9170 mL | 2.2926 mL | |
| 40 mM | 0.0688 mL | 0.3439 mL | 0.6878 mL | 1.7194 mL | |
| 50 mM | 0.0550 mL | 0.2751 mL | 0.5502 mL | 1.3756 mL | |
| 60 mM | 0.0459 mL | 0.2293 mL | 0.4585 mL | 1.1463 mL | |
| 80 mM | 0.0344 mL | 0.1719 mL | 0.3439 mL | 0.8597 mL | |
| 100 mM | 0.0275 mL | 0.1376 mL | 0.2751 mL | 0.6878 mL |