|艾替班特乙酸盐|CsnPharm

CAS No.: 138614-30-9

Icatibant acetate/艾替班特乙酸盐 Catalog No. CSN23822

Synonyms: HOE 140 acetate;Icatibant (acetate);Firazyr

Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.

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技术信息

生物活性

描述Bradykinin is a nonapeptide hormone which can increase vessel permeability, dilate blood vessels and cause smooth muscle cells to contract. Icatibant is a long acting and potent peptide antagonist of bradykinin receptor B2 with IC50 value of 1.07nM and Ki value of 0.798nM, respectively, for receptor binding studies in guinea-pig ileum preparations^[1]^[2]. Icatibant antagonized bradykinin-induced EDRF release and increase in cytosolic free calcium with IC50 value of 10nM and 1nM, respectively, in cultured bovine endothelial cells, and totally suppressed the bradykinin-induced PGI2 release from cultured endothelial cells of bovine aorta at concentration of 100nM^[1]. Also Icatibant competitively inhibited the hydrolysis of L-Ala-p-nitroanilide by recombinant aminopeptidase N with Ki value of 9.1 μM. It potentiated angiotensin III and Lys-des-Arg⁹-bradykinin in the rabbit aorta at concentration of 10–30 μM^[3]. Icatibant is usually used to treat for angioedema^[4]^[5].
参考文献

[1] Hock FJ, et al. Hoe 140 a new potent and long acting bradykinin-antagonist: in vitro studies. Br J Pharmacol. 1991 Mar;102(3):769-73.
[2] Y Arai, et al. Effect of Icatibant, a Bradykinin B2 Receptor Antagonist, on the Development of Experimental Ulcerative Colitis in Mice. Dig Dis Sci. 1999 Apr;44(4):845-51.
[3] Marie-Thérèse Bawolak, et al The Bradykinin B2 Receptor Antagonist Icatibant (Hoe 140) Blocks Aminopeptidase N at Micromolar Concentrations: Off-Target Alterations of Signaling Mediated by the Bradykinin B1 and Angiotensin Receptors. Eur J Pharmacol. 2006 Dec 3;551(1-3):108-11.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 0.7328 mL
- 3.6641 mL
- 7.3283 mL
- 5 mM
- 0.1466 mL
- 0.7328 mL
- 1.4657 mL
- 10 mM
- 0.0733 mL
- 0.3664 mL
- 0.7328 mL

技术信息

CAS号	138614-30-9	储存条件	粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C61H93N19O15S	运输	蓝冰
分子量	1364.57	别名	HOE 140 acetate;Icatibant (acetate);Firazyr;HOE-140

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Icatibant acetate/艾替班特乙酸盐 Catalog No. CSN23822

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