Icatibant (HOE-140) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.
体外研究
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).
体内研究
Icatibant (0.3, or 1.5 mg/kg, subcutaneous administration twice daily in mice) shows a significant preventive effect on ulcerative Colitis.
Animal Model:
Female mice of the CBA/J (H-2) strain.
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.
分子式
C59H89N19O13S
分子量
1304.52
CAS号
130308-48-4
中文名称
艾替班特
运输条件
Room temperature in continental US; may vary elsewhere.