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艾替班特乙酸盐 /Icatibant acetate {[allProObj[0].p_purity_real_show]}

货号:A1143118 同义名: HOE 140 acetate;Icatibant (acetate)

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.

Icatibant acetate 化学结构 CAS号:138614-30-9
Icatibant acetate 化学结构
CAS号:138614-30-9
Icatibant acetate 3D分子结构
CAS号:138614-30-9
Icatibant acetate 化学结构 CAS号:138614-30-9
Icatibant acetate 3D分子结构 CAS号:138614-30-9
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Icatibant acetate 纯度/质量文件 产品仅供科研

货号:A1143118 标准纯度: {[allProObj[0].p_purity_real_show]}
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Icatibant acetate 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].

Icatibant acetate 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.

Icatibant acetate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.73mL

0.15mL

0.07mL

3.66mL

0.73mL

0.37mL

7.33mL

1.47mL

0.73mL

Icatibant acetate 技术信息

CAS号138614-30-9
分子式C61H93N19O15S
分子量 1364.574
别名 HOE 140 acetate;Icatibant (acetate);Firazyr;HOE 140
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

溶解度

DMSO: 105 mg/mL(76.95 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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