艾替班特乙酸盐

更新时间：2026-07-09 12:29:30

艾替班特乙酸盐结构式	常用名	艾替班特乙酸盐	英文名	Icatibant acetate
	CAS号	138614-30-9	分子量	1364.57000
	密度	1.6g/cm3	沸点	N/A
	分子式	C₆₁H₉₃N₁₉O₁₅S	熔点	N/A
	MSDS	美版	闪点	N/A

艾替班特乙酸盐用途

Icatibant acetate (HOE-140 acetate) 是有效的,特异的缓激肽 B2 受体拮抗剂,IC50 和 Ki 值分别为 1.07 nM和 0.798 nM。

中文名	艾替班特醋酸盐
英文名	Icatibant acetate
中文别名	艾替班特乙酸盐
英文别名	更多

描述	Icatibant acetate (HOE-140 acetate) 是有效的,特异的缓激肽 B2 受体拮抗剂,IC50 和 Ki 值分别为 1.07 nM和 0.798 nM。
相关类别	研究领域 >> 炎症/免疫信号通路 >> G 蛋白偶联受体/G 蛋白 >> 缓激肽受体
体外研究	Icatibant(10-30μM)增强血管紧张素III,但不增强血管紧张素II(由血管紧张素AT1受体介导的收缩)和Lys-des-Arg9-缓激肽,但不能增强des-Arg9-缓激肽(缓激肽B1受体介导的作用)[3]。
体内研究	Icatibant(10-30μM)增强血管紧张素III,但不增强血管紧张素II(由血管紧张素AT1受体介导的收缩)和Lys-des-Arg9-缓激肽,但不能增强des-Arg9-缓激肽(缓激肽B1受体介导的作用)[3]。动物模型：CBA/J(H-2k)株雌性小鼠[2]。剂量：0.06、0.3或1.5mg/kg。给药：皮下给药,每日两次。结果：1.5mg/kg剂量组大鼠小肠长度为93.6±6.8mm,0.3mg/kg剂量组大肠长度为94.0±4.1mm,对缩短有明显的预防作用。
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.

密度	1.6g/cm3
分子式	C₆₁H₉₃N₁₉O₁₅S
分子量	1364.57000
精确质量	1363.68000
PSA	581.76000
LogP	1.67610
InChIKey	HKMZRZUEADSZDQ-QNQUGUDESA-N
SMILES	CC(=O)O.NC(N)=NCCCC(N)C(=O)NC(CCCN=C(N)N)C(=O)N1CCCC1C(=O)N1CC(O)CC1C(=O)NCC(=O)NC(Cc1cccs1)C(=O)NC(CO)C(=O)N1Cc2ccccc2CC1C(=O)N1C(C(=O)NC(CCCN=C(N)N)C(=O)O)CC2CCCCC21
外观性状	粉末
储存条件	-20℃

个人防护装备	Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
危险品运输编码	NONH for all modes of transport

Contribution of endogenous bradykinin to fibrinolysis, inflammation, and blood product transfusion following cardiac surgery: a randomized clinical trial.

Clin. Pharmacol. Ther. 93(4) , 326-34, (2013)

Bradykinin increases during cardiopulmonary bypass (CPB) and stimulates the release of nitric oxide, inflammatory cytokines, and tissue-type plasminogen activator (t-PA), acting through its B2 recepto...

Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells.

Am. J. Physiol. Cell Physiol. 303(12) , C1260-8, (2012)

In this study, the interaction of natriuretic peptides (NP) and bradykinin (BK) signaling pathways was identified by measuring membrane potential (V(m)) and intracellular Ca(2+) using the patch-clamp ...

Influence of kinin peptides on monocyte-endothelial cell adhesion.

J. Cell. Biochem. 115(11) , 1985-95, (2014)

Adhesion of leukocytes to vascular endothelium in response to proinflammatory mediators is an important component of the overall inflammatory reaction. In the current work, we used a retinoic acid-dif...

Icatibant acetate