CAS 138614-30-9|Icatibant acetate
| Common Name | Icatibant acetate | ||
|---|---|---|---|
| CAS Number | 138614-30-9 | Molecular Weight | 1364.57000 |
| Density | 1.6g/cm3 | Boiling Point | / |
| Molecular Formula | C61H93N19O15S | Melting Point | / |
| MSDS | USA | Flash Point | / |
Names
| Name | Icatibant acetate |
|---|---|
| Synonym | More Synonyms |
Icatibant acetate BiologicalActivity
| 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/ImmunologySignaling 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. |
Chemical & Physical Properties
| Density | 1.6g/cm3 |
|---|---|
| Molecular Formula | C61H93N19O15S |
| Molecular Weight | 1364.57000 |
| Exact Mass | 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 |
| Storage condition | -20℃ |
Safety Information
| Personal Protective Equipment | Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter |
|---|---|
| RIDADR | NONH for all modes of transport |
Articles34
More Articles| 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... |
Synonyms
| Icatibant acetate |
