Icatibant , 98% , 130308-48-4

Synonym(s):
;Icatibant acetate

CAS NO.：130308-48-4

Empirical Formula: C59H89N19O13S

Molecular Weight: 1304.52

MDL number: MFCD00213940

PRODUCT Properties

• Density: 1.60±0.1 g/cm3(Predicted)
• storage temp.: Sealed in dry,2-8°C
• solubility: Water:100.0(Max Conc. mg/mL);76.66(Max Conc. mM)
• form: powder
• pka: 3.60±0.21(Predicted)
• color: white
• Water Solubility: Soluble to 1 mg/ml in water
• Sequence: H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH
• InChIKey: QASONHYHOCRAHL-DOMVFXHKSA-N
• CAS DataBase Reference: 130308-48-4

Description and Uses

Hoe 140 (D-Arg-[Hyp3, Thi5, D-Tic7, Oic8]-bradykinin), on bradykinin- and platelet-activating factor (PAF)-induced bronchoconstriction and airway microvascular leakage in anesthetized guinea pigs. Hoe 140 is highly potent and long-acting in inhibiting BK-induced hypotensive responses in the rat. Four hours after s.c. administration of 20nmol kg-1, inhibition still amounted to 60% whereas the effect of 200nmol kg-1 of d-Arg-[Hyp2, Thi5,8, d-Phe7]BK was not significant[1-2].

Icatibant is an antagonist of the human bradykinin B2 receptor (B2R), that can be used for the treatment of hereditary angioedema (HAE). Upon administration, icatibant targets and binds to B2R, thereby preventing bradykinin from binding to the B2R. This may prevent bradykinin/B2R-mediated vasodilation, the resulting increase in vascular permeability, and the swelling, inflammation, and pain associated with HAE. This may also prevent or improve pulmonary edema not associated with HAE and improve the associated decrease in blood oxygen levels.

Safety

• WGK Germany: 3