| Bosentan Hydrateendothelin receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 99.25%
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| Cas No. | 157212-55-0 | SDF | Download SDF |
| Synonyms | N/A | ||
| Chemical Name | 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide;hydrate | ||
| Canonical SMILES | CC(C)(C)C1=CC=C(C=C1)S(=O)(=O)NC2=C(C(=NC(=N2)C3=NC=CC=N3)OCCO)OC4=CC=CC=C4OC.O | ||
| Formula | C27H31N5O7S | M.Wt | 569.63 |
| Solubility | ≥28.5mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: Inhibiting endothelin receptor A and B with an IC50 of 15.1 ± 1.6 μM in P388/dx cells.
A sulfonamide-derived, competitive and specific endothelin receptor antagonist with a relatively higher affinity to the endothelin A receptor than endothelin B receptor. By competitively binding to endothelin A and endothelin B receptors in the endothelium and vascular smooth muscle, Bosentan offset the effect of endothelin which is an extremely potent endogenous vasoconstrictor and broncho-constrictor. In addition, Bosentan decreases both pulmonary and systemic vascular resistance and is particularly applied in the treatment of pulmonary arterial hypertension. [1]
In vitro: A study was performed in vitro to measure the influence of Bosentan on the angiogenic performance of dermal microvascular endothelial cells (MVECs) and to detect the capacity of Bosentan in offsetting the antiangiogenic effects of systemic sclerosis sera. It was found that Bosentan significantly increased cell viability and offset the antiangiogenic effects of systemic sclerosis sera on dermal MVECs. [2]
In vivo: A study was conducted to investigate the effect of Bosentan on plasma leptin level after myocardial infarction in Wistar rats. After oral administration of Bosentan once daily at the dose of 100 mg/kg for 2 days, concentration of leptin in plasma significantly increased. This finding revealed that Bosentan played an crucial role on regulating leptin concentration in ischemic cardiovascular pathology. [1]
Clinical trials: A double-blind, placebo-controlled clinical trial was conducted to study the effect of bosentan on exercise capacity in a larger number of patients. 213 patients with pulmonary arterial hypertension were administered with 62.5 mg Bosentan twice daily for 4 weeks followed by either of two doses of Bosentan (125 or 250 mg twice daily) for a minimum of 12 weeks. It was found that 125 mg Bosentan was well tolerated and beneficial in patients with pulmonary arterial hypertension. [3]
References:[1] Ostrowski RP, Januszewski SA, Kowalska ZA and Kapuscinski A. Effect of endothelin receptor antagonist bosentan on plasma leptin concentration in acute myocardial infarction in rats. Pathophysiology. 2003 Sep; 9(4): 249-56.[2]Romano E, Bellando-Randone S, Manetti M, Bruni C, Lepri G, Matucci-Cerinic M, Guiducci S. Bosentan blocks the antiangiogenic effects of sera from systemic sclerosis patients: an in vitro study. Clin Exp Rheumatol. 2015 Aug; 33(4 Suppl 91): S148-52. [3]Rubin LJ, Badesch DB, Barst RJ, Galiè N, Black CM et, al. Bosentan therapy for pulmonary arterial hypertension. New Engl J Med. 2002 Mar; 346 (12): 896-903.
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3.预冻结果的不同，使冻干曲线对于每瓶产品未必都是合适，会出现产品干燥效果不一的情况。
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冻干机型号不一样，价格也不一致；
便宜些的也在一万左右。
过去是完全由自动化代替人工，现在看来完全代替人工是太理想化，还需要一定的时间，在智能制造流程中，人虽然不再负责提供劳动工作，但仍然扮演生产过程的设计决策者，以及流程的管理者。拓纷HFD系列小型真空冷冻干燥机将具有智能化、无人化、信息化等特性，这类自动化智能化小型冷冻干燥机将能将设备和物料信息联结在一起，用户能快速处理各地物料冻干需求。
大连双瑞科技（09年成立，针对制药行业的）
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