Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Bosentan hydrate (Ro 47-0203) 是endothelin-1 (ET)竞争性拮抗剂,在人SMC 细胞中,它能够作用于 ETA 受体(Ki:4.7 nM)和 ETB 受体(Ki:95 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
10 mg | ¥ 225 | 现货 | ||
25 mg | ¥ 347 | 现货 | ||
50 mg | ¥ 578 | 现货 | ||
100 mg | ¥ 970 | 现货 | ||
200 mg | ¥ 1,660 | 现货 | ||
500 mg | ¥ 2,920 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 613 | 现货 |
产品描述 | Bosentan hydrate (Ro 47-0203) is a competitive and dual antagonist of endothelin-1 at the endothelin-A (ET-A) and endothelin-B (ET-B) receptors. |
靶点活性 | ETB:95 nM(Ki), ETA:4.7 nM(Ki) |
体外活性 | Bosentan competitively antagonizes the specific binding of [125 I]-labeled ET-1 on human smooth muscle cells (ET-A receptors)human placenta (ET-B receptors). Bosentan also inhibits the binding of selective ET-B ligands on porcine trachea. Contractions induced by ET-1 in isolated rat aorta (ET-A) and by the selective ET-B agonist sarafotoxin S6C in rat trachea are competitively inhibited by Bosentan (pA2= 7.2 and 6.0, respectively), as is the endothelium-dependent relaxation to sarafotoxin S6C in rabbit superior mesenteric artery (pA2= 6.7). The binding of 40 other peptides, prostaglandins, ions and neurotransmitters is not significantly affected by Bosentan, which shows its specificity for ET receptors. [1] |
体内活性 | Bosentan inhibits the presser response to big ET-1 both after i.v. and oral administration, with a long duration of action and no intrinsic agonist activity. Bosentan also inhibits the depressor and presser effect of ET-1 and sarafotoxin S6C. Its pharmacological profile makes Bosentan a potentially useful drug in the management of clinical disorders associated with vasoconstriction.[1] Bosentan is the first oral non-peptide mixed ETA/B-receptor antagonist. Long-term treatment with Bosentan has markedly increased the survival, hemodynamics, and cardiac remodeling in rats with CHF. Bosentan decreases arterial BP to a similar degree as an angiotensin-converting enzyme (ACE) inhibitor. Administration of Bosentan in rats with CHF after acute MI significantly decreases arterial BP and has additive effect to that of an ACE inhibitor. Acute and chronical treatment with Bosentan also improves the systemic and pulmonary hemodynamics by a decrease in peripheral and pulmonary vascular resistance, and increase of cardiac output in patients with CHF. [2] |
细胞实验 | Bosentan is prepared in DMSO and diluted with appropriate medium before use[2]. Cell viability is evaluated by the trypan blue exclusion test. Human dermal fibroblasts are treated with the indicated concentration of Bosentan (10, 20 and 40 μM). Cell viability is examined at 24 and 48 hours. Stained (dead) and unstained (viable) cells are counted with a hematocytometer[2]. |
别名 | 波生坦水合物, Bosentan Hydrate, Benzenesulfonamide, Actelion, Ro 47-0203 |
分子量 | 569.63 |
分子式 | C27H29N5O6S·H2O |
CAS No. | 157212-55-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (163.3 mM)
Ethanol: 2 mg/mL (3.51 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.7555 mL | 8.7776 mL | 17.5553 mL | 43.8881 mL |
DMSO | 5 mM | 0.3511 mL | 1.7555 mL | 3.5111 mL | 8.7776 mL |
10 mM | 0.1756 mL | 0.8778 mL | 1.7555 mL | 4.3888 mL | |
20 mM | 0.0878 mL | 0.4389 mL | 0.8778 mL | 2.1944 mL | |
50 mM | 0.0351 mL | 0.1756 mL | 0.3511 mL | 0.8778 mL | |
100 mM | 0.0176 mL | 0.0878 mL | 0.1756 mL | 0.4389 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Bosentan (hydrate) 157212-55-0 GPCR/G Protein Endothelin Receptor 波生坦水合物 Bosentan Bosentan Hydrate inhibit Benzenesulfonamide Inhibitor Actelion Ro 47-0203 inhibitor