| 货号 | 15783-1mg |
| 描述 | The anaphylatoxin C3a induces a range of responses by activating its G protein-coupled receptor, C3aR, resulting in calcium mobilization.1 SB 290157 is a non-peptide antagonist of C3aR, competitively blocking C3a binding with an IC50 value of 200 nM.2 It potently inhibits a wide variety of C3a-induced responses in cells, including calcium increase in human neutrophils (IC50 = 28 nM) and ATP release from guinea pig platelets (IC50 = 30 nM).2 SB 290157 is also effective in vivo, reducing inflammation in a variety of animal models.2,3,4 It also significantly reduces or reverses diet-induced obesity in rats and accelerates the mobilization of hematopoietic progenitor cells to the peripheral blood in mice.5,6 Notably, SB 290157 has C3aR agonist activity in some cell systems.7,8 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ames, R.S.,Li, Y.,Sarau, H.M., et al. Molecular cloning and characterization of the human anaphylatoxin C3a receptor. The Journal of Biological Chemisty 271(34), 20231-20234 (1996). 2.Ames, R.S.,Lee, D.,Foley, J.J., et al. Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models. Journal of Immunology 166(10), 6341-6348 (2001). 3.Proctor, L.M.,Arumugam, T.V.,Shiels, I., et al. Comparative anti-inflammatory activities of antagonists to C3a and C5a receptors in a rat model of intestinal ischaemia/reperfusion injury. British Journal of Pharmacology 142(4), 756-764 (2004). 4.Hutamekalin, P.,Takeda, K.,Tani, M., et al. Effect of the C3a-receptor antagonist SB 290157 on anti-OVA polyclonal antibody-induced arthritis. Journal of Pharmacological Sciences 112(1), 56-63 (2010). 5.Lim, J.,Iyer, A.,Suen, J.Y., et al. C5aR and C3aR antagonists each inhibit diet-induced obesity, metabolic dysfunction, and adipocyte and macrophage signaling. The FASEB Journal 27(2), 822-831 (2013). 6.Ratajczak, J.,Reca, R.,Kucia, M., et al. Mobilization studies in mice deficient in either C3 or C3a receptor (C3aR) reveal a novel role for complement in retention of hematopoietic stem/progenitor cells in bone marrow. Blood 103(6), 2071-2078 (2004). 7.Mathieu, M.C.,Sawyer, N.,Greig, G.M., et al. The C3a receptor antagonist SB 290157 has agonist activity. Immunology Letters 100(2), 139-145 (2005). 8.Therien, A.G. Agonist activity of the small molecule C3aR ligand SB 290157. Journal of Immunology 174(12), 7479-7490 (2005). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 526.5 |
| 分子式 | C22H28N4O4 • CF3COOH |
| CAS号 | 1140525-25-2 |
| 稳定性 | ≥ 2 years |
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