Bosentan Hydrate
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50值:在P388/dx细胞中抑制内皮素受体A和B,IC50值为15.1 ± 1.6 μM。
一种磺酰胺衍生的、竞争性和特异性内皮素受体拮抗剂,与内皮素B受体相比,它对内皮素A受体具有相对更高的亲和力。通过在内皮细胞和血管平滑肌细胞中与内皮素A和内皮素B受体竞争性结合,波生坦(Bosentan)可抵消内皮素的作用,而内皮素是非常有效的内源性血管收缩剂和支气管收缩剂。此外,Bosentan减少肺和全身血管阻力,尤其用于治疗肺动脉高压[1]。
体外实验:进行体外研究,检测Bosentan对真皮微血管内皮细胞(MVECs)的血管生成性能的影响,并检测Bosentan在抵消系统性硬化症血清的抗血管生成作用的能力。研究发现,Bosentan显著增强细胞活力,抵消系统性硬化症血清对真皮微血管内皮细胞的抗血管生成作用[2]。
体内实验:进行一项研究,调查Wistar大鼠心肌梗死后,Bosentan对血浆瘦素水平的作用。每日一次连续两天口服100 mg/kg的Bosentan后,血浆内瘦素浓度显著增加。该研究表明,Bosentan在调节缺血性心血管病变的瘦素浓度上具有重要作用[1]。
临床试验:进行一项双盲和安慰剂对照临床试验,在大量的病人体内研究bosentan对运动能力的作用。给213名患有肺动脉高压的病人连续4周每天两次服用62.5 mg的bosentan,然后至少连续12周每天两次服用125 mg或250 mg剂量的bosentan。研究发现,125 mg的bosentan耐受性良好,且对肺动脉高压患者有益[3]。
参考文献:
[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.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 569.63 |
Cas No. | 157212-55-0 |
Formula | C27H31N5O7S |
Solubility | ≥57.21 mg/mL in DMSO; insoluble in H2O; ≥2.45 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 4-tert-butyl-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-ylpyrimidin-4-yl]benzenesulfonamide;hydrate |
SDF | Download SDF |
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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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