Icatibant acetate

[Description]:

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[1][2][3].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> GPCR/G Protein >> Bradykinin Receptor

[In Vitro]

Icatibant (10-30 μM) potentiates angiotensin III, but not angiotensin II (contraction mediated by angiotensin AT1 receptors), and Lys-des-Arg9-bradykinin, but not des-Arg9-bradykinin (effects mediated by the bradykinin B1 receptors)[3].

[In Vivo]

Icatibant (10-30 μM) potentiates angiotensin III, but not angiotensin II (contraction mediated by angiotensin AT1 receptors), and Lys-des-Arg9-bradykinin, but not des-Arg9-bradykinin (effects mediated by the bradykinin B1 receptors)[3]. Animal Model: Female mice of the CBA/J (H-2k) strain[2]. Dosage: 0.06, 0.3, or 1.5 mg/kg. Administration: Subcutaneous administration twice daily. Result: The length of the large intestine was 93.6±6.8 mm with the 1.5 mg/kg dosage and 94.0±4.1 mm with the 0.3 mg/kg dosage , showing a significant preventive effect on shortening.

[References]

[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.

[ Density]:
1.6g/cm3

[ Molecular Formula ]:
C₆₁H₉₃N₁₉O₁₅S

[ Molecular Weight ]:
1364.57000

[ Exact Mass ]:
1363.68000

[ PSA ]:
581.76000

[ LogP ]:
1.67610

[ Storage condition ]:
-20℃

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
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...

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