Daltroban
Based on 1 Customer Validation
Daltroban (BM-13505) is a selective and specific thromboxane A2 (TXA2) receptor antagonist. Daltroban increase intracellular calcium in vascular smooth muscle cells. Daltroban shows protective effect in reperfusion injury.
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 : 98.19%
- CAS 番号: 79094-20-5
- 分子式: C16H16ClNO4S
- 分子量:353.82
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
製品説明
IC50 & Target
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TXA2 |
体内実験
In comparison with vehicle (physiological saline)-treated cats, Daltroban (20 mg/kg per hour i.v.) reduces the ischaemia-induced rise in the ST segment and prevented the development of a Q-wave in the ECG during reperfusion. Daltroban protects the myocardium from ischaemic injury and that this effect involves prevention of ischaemia-induced leukocytosis[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male cats (2.8 to 4.6 kg; anesthetized cat model)[2]
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Dosage:1 mg/kg
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Administration:i.v.; 30 minutes before reperfusion at a rate of 1 mg/kg followed by 1 mg/kg/hour
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Result:Significantly reduced the area of ischemic tissue as a percent of total left ventricular mass and total area at risk, without altering basic hemodynamics and thereby not influencing myocardial oxygen demand.
化学情報
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CAS 番号 79094-20-5
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性状 Solid
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分子量 353.82
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分子式 C16H16ClNO4S
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Color White to light yellow
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SMILES
O=C(CC1=CC=C(C=C1)CCNS(=O)(C2=CC=C(C=C2)Cl)=O)O
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別名
BM-13505; SKF 96148
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°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
体外:
DMSO : 22 mg/mL (62.18 mM; Need ultrasonic and warming; 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)
プロトコル
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Calcium Spark Assay
Calcium sparks are localized, transient increases in intracellular calcium concentration ([Ca2+]i) that occur in cardiac myocytes and represent elementary events underlying excitation-contraction coupling. These events are generated by the coordinated opening of clusters of ryanodine receptors (RyRs) on the sarcoplasmic reticulum membrane, leading to a brief release of Ca2+ into the cytosol. The detection and analysis of calcium sparks provide insights into the mechanisms of calcium handling and signaling in cardiac cells. Imaging techniques using fluorescent calcium indicators such as Fluo-3 are employed to visualize these subcellular calcium transients with high spatial and temporal resolution. The protocol is based on established methodologies described in primary literature for both experimental measurement and automated analysis of calcium sparks.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
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 (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Miki I, et al. Differences in activities of thromboxane A2 receptor antagonists in smooth muscle cells. Eur J Pharmacol. 1992 Oct 1;227(2):199-204. [Content Brief]
[2]. Thiemermann C, et al. The thromboxane receptor antagonist, daltroban, protects the myocardium from ischaemic injury resulting in suppression of leukocytosis. Eur J Pharmacol. 1988 Oct 11;155(1-2):57-67. [Content Brief]
[3]. Bhat AM, et al. Protective effect of the specific thromboxane receptor antagonist, BM-13505, in reperfusion injury following acute myocardial ischemia in cats. Am Heart J. 1989 Apr;117(4):799-803. [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 | 2.8263 mL | 14.1315 mL | 28.2630 mL | 70.6574 mL |
| 5 mM | 0.5653 mL | 2.8263 mL | 5.6526 mL | 14.1315 mL | |
| 10 mM | 0.2826 mL | 1.4131 mL | 2.8263 mL | 7.0657 mL | |
| 15 mM | 0.1884 mL | 0.9421 mL | 1.8842 mL | 4.7105 mL | |
| 20 mM | 0.1413 mL | 0.7066 mL | 1.4131 mL | 3.5329 mL | |
| 25 mM | 0.1131 mL | 0.5653 mL | 1.1305 mL | 2.8263 mL | |
| 30 mM | 0.0942 mL | 0.4710 mL | 0.9421 mL | 2.3552 mL | |
| 40 mM | 0.0707 mL | 0.3533 mL | 0.7066 mL | 1.7664 mL | |
| 50 mM | 0.0565 mL | 0.2826 mL | 0.5653 mL | 1.4131 mL | |
| 60 mM | 0.0471 mL | 0.2355 mL | 0.4710 mL | 1.1776 mL |