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

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

Icatibant acetate是一个强效且特异性的肽类拮抗剂,作用于 bradykinin B2 受体,IC50 和 Ki 值分别为 1.07 nM 和 0.798 nM。

Icatibant acetate/艾替班特乙酸盐 化学结构 CAS号:138614-30-9
Icatibant acetate/艾替班特乙酸盐 化学结构
CAS号:138614-30-9
Icatibant acetate/艾替班特乙酸盐 3D分子结构
CAS号:138614-30-9
Icatibant acetate/艾替班特乙酸盐 化学结构 CAS号:138614-30-9
Icatibant acetate/艾替班特乙酸盐 3D分子结构 CAS号:138614-30-9
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Icatibant acetate/艾替班特乙酸盐 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/艾替班特乙酸盐 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/艾替班特乙酸盐 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/艾替班特乙酸盐 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/艾替班特乙酸盐 技术信息

CAS号138614-30-9
分子式C61H93N19O15S
分子量 1364.57
SMILES Code CC(O)=O.O=C(N1[C@@]2([C@]([H])(C[C@H]1C(N[C@@H](CCCNC(N)=N)C(O)=O)=O)CCCC2)[H])[C@@H]3N(C([C@@H](NC([C@H](CC4=CC=CS4)NC(CNC([C@H]5N(C([C@H]6N(C([C@@H](NC([C@@H](CCCNC(N)=N)N)=O)CCCNC(N)=N)=O)CCC6)=O)C[C@@H](C5)O)=O)=O)=O)CO)=O)CC7=CC=CC=C7C3
MDL No. MFCD04112967
别名 HOE 140 acetate; Icatibant (acetate); Firazyr; HOE 140
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

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

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