Icatibant (acetate) (HOE-140 acetate) 是一种有效的特异性缓激肽 B2 受体肽拮抗剂，IC50 和 Ki 分别为 1.07 nM 和 0.798 nM。
| Cas No. | 138614-30-9 |
| 别名 | 艾替班特乙酸盐,HOE 140 acetate |
| Canonical SMILES | O=C(N1[C@](CCCC2)([H])[C@]2([H])C[C@H]1C(N[C@H](C(O)=O)CCCNC(N)=N)=O)[C@@H]3N(C([C@H](CO)NC([C@H](CC4=CC=CS4)NC(CNC([C@@H]5C[C@@H](O)CN5C([C@H]6N(C([C@@H](NC([C@H](N)CCCNC(N)=N)=O)CCCNC(N)=N)=O)CCC6)=O)=O)=O)=O)=O)CC7=C(C=CC=C7)C3.OC(C)=O |
| 分子式 | C59H89N19O13S•XC2H4O2 |
| 分子量 | 1304.5 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 0.25 mg/ml,PBS (pH 7.2): 10 mg/ml |
| 储存条件 | -20°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Icatibant is a synthetic peptide antagonist of the bradykinin B2 receptor with IC50 and Ki values of 1.07 and 0.798 nM, respectively, in guinea pig ileal cell membranes. It inhibits bradykinin-induced contractions in isolated guinea pig ileum and pulmonary arteries as well as in rat uterus (IC50s = 11, 5.4, and 4.9 nM, respectively). In vivo, icatibant inhibits bronchoconstriction induced by bradykinin in a guinea pig model (ID50s = 13.4 and 31.8 pmol/kg, i.v., for pulmonary resistance and dynamic lung compliance, respectively). Icatibant (30 µg, i.v.) also reduces vascular permeability in the footpad and intestine in a mouse model of hereditary angioedema. Formulations containing icatibant have been used for the treatment of hereditary angioedema. |
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