Icatibant

• CAT Number: I001158
• CAS Number: 130308-48-4
• Molecular Formula: C59H89N19O13S
• Molecular Weight: 1304.52
• Purity: ≥95%
• Target: Bradykinin Receptors
• Solubility: 10 mM in H2O
• Storage: Store at -20C
• IC50: 1.07 nM [1]

Icatibant(HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.IC50 value: 1.07 nM [1]Target: bradykinin B2 receptor antgonistin vitro: In receptor binding studies in guinea-pig ileum preparations, Hoe 140 showed an IC50 of 1.07 x 10(-9) mol l-1 and a KI value of 7.98 x 10(-10) mol l-1. In isolated organ preparations Hoe 140 and D-Arg-[Hyp2,Thi5,8, D-Phe7]BK inhibited bradykinin-induced contractions concentration dependently, with IC50-values in the guinea-pig ileum preparation of 1.1 x 10(-8) mol l-1 and 3 x 10(-5) mol l-1, respectively. pA2 values in this tissue were 8.42 and 6.18, respectively [1].in vivo: HOE 140 (1, 3, or 10 μg/10 μl physiological saline) was administered into the wound by a sterile micropipette. HOE 140 (1, 3, 10 μg) significantly relieved mechanical allodynia and guarding in comparison with vehicle-treated group [2]. HOE-140 (10 nmol/kg) protected against memory impairment. This treatment attenuated the brain edema, interleukin-1β, tumor necrosis factor-α, and nitric oxide metabolites content elicited by mLFPI. Accordingly, HOE-140 administration protected against the increase of nicotinamide adenine dinucleotide phosphate oxidase activity, thiobarbituric-acid-reactive species, protein carbonylation generation, and Na+ K+ ATPase inhibition induced by trauma [3].

Reference

1:The Icatibant Outcome Survey: experience of hereditary angioedema management from six European countries. Caballero T, Aberer W, Longhurst HJ, Maurer M, Zanichelli A, Perrin A, Bouillet L, Andresen I; IOS Study Group..J Eur Acad Dermatol Venereol. 2017 Apr 1. doi: 10.1111/jdv.14251. [Epub ahead of print] PMID: 28370444 2:Hereditary angioedema with normal C1 inhibitor in a French cohort: Clinical characteristics and response to treatment with icatibant. Bouillet L, Boccon-Gibod I, Launay D, Gompel A, Kanny G, Fabien V, Fain O; IOS Study Group..Immun Inflamm Dis. 2017 Jan 11;5(1):29-36. doi: 10.1002/iid3.137. eCollection 2017 Mar. PMID: 28250922 Free PMC Article3:Comparing acquired angioedema with hereditary angioedema (types I/II): findings from the Icatibant Outcome Survey. Longhurst HJ, Zanichelli A, Caballero T, Bouillet L, Aberer W, Maurer M, Fain O, Fabien V, Andresen I; IOS Study Group..Clin Exp Immunol. 2017 Apr;188(1):148-153. doi: 10.1111/cei.12910. Epub 2017 Feb 9. PMID: 27936514 Free PMC Article4:Long-term safety of icatibant treatment of patients with angioedema in real-world clinical practice. Zanichelli A, Maurer M, Aberer W, Caballero T, Longhurst HJ, Bouillet L, Fabien V, Andresen I; IOS Study Group..Allergy. 2017 Jun;72(6):994-998. doi: 10.1111/all.13103. Epub 2017 Mar 13. PMID: 27926986 5:Subcutaneous Icatibant for the Treatment of Hereditary Angioedema Attacks: Comparison of Home Self-Administration with Administration at a Medical Facility. Otani IM, Lumry WR, Hurwitz S, Li HH, Craig TJ, Holtzman NS, Iandoli MI, Tucker J, Riedl MA, Zuraw BL, Banerji A.J Allergy Clin Immunol Pract. 2017 Mar – Apr;5(2):442-447.e1. doi: 10.1016/j.jaip.2016.09.023. Epub 2016 Nov 3. PMID: 27818136 6:Icatibant Compared to Steroids and Antihistamines for ACE-Inhibitor-Induced Angioedema. Botnaru T, Robert A, Mottillo S.CJEM. 2017 Mar;19(2):159-162. doi: 10.1017/cem.2016.21. Epub 2016 May 18. PMID: 27189625 7:Pharmacokinetics of single and repeat doses of icatibant. Leach JK, Spencer K, Mascelli M, McCauley TG.Clin Pharmacol Drug Dev. 2015 Mar;4(2):105-11. doi: 10.1002/cpdd.138. Epub 2015 Feb 2. PMID: 27128215 8:Icatibant as acute treatment for hereditary angioedema in adults. Farkas H.Expert Rev Clin Pharmacol. 2016 Jun;9(6):779-88. doi: 10.1080/17512433.2016.1182425. Epub 2016 May 13. Review. PMID: 27123689 9:The Icatibant Outcome Survey: treatment of laryngeal angioedema attacks. Longhurst HJ, Aberer W, Bouillet L, Caballero T, Maurer M, Fabien V, Zanichelli A; IOS Study Group..Eur J Emerg Med. 2016 Jun;23(3):224-7. doi: 10.1097/MEJ.0000000000000292. PMID: 27116379 Free PMC Article10:First report of icatibant treatment in a pregnant patient with hereditary angioedema. Farkas H, Kőhalmi KV, Veszeli N, Tóth F, Varga L.J Obstet Gynaecol Res. 2016 Aug;42(8):1026-8. doi: 10.1111/jog.13003. Epub 2016 Apr 19. PMID: 27093898