| 货号 | 5473/1 |
| 供应商 | Tocris |
| 生物活性 | Potent C5a receptor antagonist (IC50 = 20 nM). Also MrgX2 agonist. Stimulates MrgX2-mediated mast cell degranulation. Also inhibits C5a-induced hypernociception in rats, inhibits lung metastasis in a mouse breast cancer model and reduces atherosclerotic lesions in a mouse model of atherosclerosis. |
| 运输条件 | Blue Ice |
| 存放说明 | -20℃ |
| 计算分子量 | 896.1 |
| 分子式 | C47H65N11O7< |
| 可溶性/溶解性 | Soluble to 2 mg/ml in water |
| 序列号 | FXPXWR (Modifications: Phe-1 = N-terminal Ac, X-2 = Orn, X-4 = D-Cha, Lactam bridge: Orn-2 to Arg-6 ) |
| 参考文献 | Vadrevuet al (2014) Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Cancer Res. 74 3454. PMID: 24786787. Mantheyet al (2011) Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. FASEB J 25 2447. PMID: 21490292. Subramanianet al (2011) PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Mol.Pharmacol. 79 1005. PMID: 21441599. Tinget al (2008) Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Br.J.Pharmacol. 153 1043. PMID: 18084313. Finchet al (1999) Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. J.Med.Chem. 42 1965. PMID: 10354404. |