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Icatibant acetate

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Chemical Structure| 138614-30-9 同义名 : HOE 140 acetate;Icatibant (acetate);Firazyr;HOE 140
CAS号 : 138614-30-9
货号 : A1143118
分子式 : C61H93N19O15S
纯度 : 98+%
分子量 : 1364.574
MDL号 : MFCD04112967
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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.