Ambrisentan
- 安倍生坦;BSF 208075;LU 208075
货号: abs813296
货号-规格 | 货期 | 价格 | 数量 |
abs813296-5mg | 1-2周 | ¥522.00 | - + |
abs813296-10mg | 1-2周 | ¥1345.00 | - + |
abs813296-20mg | 1-2周 | ¥2084.00 | - + |
abs813296-50mg | 1-2周 | ¥2305.00 | - + |

产品描述 | ||
描述 | Ambrisentan是一种高选择性的内皮素-1A型受体拮抗剂,IC50为18 nM,用于治疗肺动脉高血压(PAH)。 | |
纯度 | >98% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
别名 | 安倍生坦;BSF 208075;LU 208075 | |
可溶性/溶解性 | Ethanol :21 mg/mL (55.5 mM)
DMSO :71 mg/mL (187.6 mM) | |
生物活性 | ||
靶点 | ET-A | |
In vitro(体外研究) | Ambrisentan only increases intracellular calcein fluorescence in P388/dx cells at concentrations above 100 μM and in L-MDR1 cells not at all indicating negligible P-gp inhibition. Ambrisentan inhibits specific ET-1 binding in these tissues in a concentration-dependent manner. Ambrisentan undergoes oxidative metabolism mainly by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP3A5 and CYP2C19. Ambrisentan is not only a strong inducer of CYP3A4, but also of ABCB1 and ABCG2. Ambrisentan also has a concentration-dependent effect on PXR activity, but because plateau effects are not reached, an EC50-value could not be calculated. Ambrisentan inhibits specific ET-1 binding in a concentration-dependent manner at nanomolar ranges of IC50. Ambrisentan significantly increases the dissociation constant for bladder ET-1 binding without affecting maximal number of binding sites (Bmax). Ambrisentan seem to bind to bladder ET-1 receptor in a competitive and reversible manner. Ambrisentan is an effective and safe treatment which is a valuable addition to the armamentarium against PAH. Ambrisentan offers a relative lack of drug interactions, once daily dosing and reassuring liver safety, offering safety and convenience advantages over bosentan. | |
In vivo(体内研究) | In the Ambrisentan group, hepatic hydroxyproline content is significantly lower than in the control group (18.0 μg/g±6.1 μg/g vs 33.9 μg/g±13.5 μg/g liver, respectively, P=0.014). Hepatic fibrosis estimated by Sirius red staining and areas positive for α-smooth muscle actin, indicative of activated hepatic stellate cells, are also significantly lower in the Ambrisentan group (0.46%±0.18% vs 1.11%±0.28%, respectively, P=0.0003; and 0.12%±0.08% vs 0.25%±0.11%, respectively, P=0.047). Moreover, hepatic RNA expression levels of procollagen-1 and tissue inhibitor of metalloproteinase-1 (TIMP-1) are significantly lower by 60% and 45%, respectively, in the Ambrisentan group. Inflammation, steatosis, and endothelin-related mRNA expression in the liver are not significantly different between the groups. Ambrisentan attenuates the progression of hepatic fibrosis by inhibiting hepatic stellate cell activation and reducing procollagen-1 and TIMP-1 gene expression. Ambrisentan did not affect inflammation or steatosis. | |
参考文献 | ||
参考文献 | Long-term ambrisentan therapy for the treatment of pulmonary arterial hypertension. Oudiz RJ,et al. J Am Coll Cardiol. 2009 Nov 17;54(21):1971-81. PMID: 1990987 䔸Żᩄ 族痛셌Ų 族痛셌Ų Item 褐 Count ๏ 趌๐ 侮靴 ᠠi S ñ ñ 眘⮦眀⮦敲痛๏ࠃ 馸鳘祖Item Count 3 ᬴叫㺍痭ᠠ靴i 縉 靴蘿敌ଧ靴ᠠi ᭰叫㺍痭ᡸ顴먲 | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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