| 货号 | 10009835-1mg |
| 描述 | MK-0524 is a potent, selective prostaglandin D2(PGD2)receptor DP1 antagonist with Ki values of 0.57 nM and 0.75 µM for the DP1 and DP2 receptors, respectively.1 It inhibits PGD2-induced accumulation of cAMP in both washed platelets and platelet-rich plasma with IC50 values of 0.09 and 4.0 nM, respectively.1 In a sheep model of allergic rhinitis, 0.1 mg/kg MK-0524 completely blocked PGD2-induced nasal congestion.1 At a dose of 4 mg/kg, MK-0524 suppressed a nicotinic acid-induced vasodilatory response by 80% in a mouse model of flushing, an undesirable side-effect of niacin treatment for dyslipidemia.2 In an in vitro model of amyotrophic lateral sclerosis, MK-0524 has been shown to partially protect cultured motor neurons from PGD2-induced toxicity.3,4 |
| 别名 | Laropiprant; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Sturino, C.F.,ONeill, G.,Lachance, N., et al. Discovery of a potent and selective prostaglandin D2 receptor antagonist, [(3R)-4-(4-chloro-benzyl)-7-fluoro-5-(methylsulfonyl)-1,2,3,4-tetrahydrocyclopental[b]indol-3-yl]-acetic acid. Journal of Medicinal Chemistry 50, 794-806 (2007). 2.Cheng, K.,Wu, T.J.,Wu, K.K., et al. Antagonism of the prostaglandin D2 receptor 1 suppresses nicotinic acid-induced vasodilation in mice and humans. Proceedings of the National Academy of Sciences of the United States of America 103(17), 6682-6687 (2006). 3.Marchetto, M.C.N.,Muotri, A.R.,Mu, Y., et al. Non-cell-autonomous effect of human SOD1G37R astrocytes on motor neurons derived from human embryonic stem cells. Cell. Stem Cell 3(6), 649-657 (2008). 4.Di Giorgio, F.P.,Boulting, G.L.,Bobrowicz, S., et al. Human embryonic stem cell-derived motor neurons are sensitive to the toxic effect of glial cells carrying an ALS-causing mutation. Cell. Stem Cell 3(6), 637-648 (2008). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 435.9 |
| 分子式 | C21H19ClFNO4S |
| CAS号 | 571170-77-9 |
| 稳定性 | ≥ 2 years |
| 本官网所有报价均为常温或者蓝冰运输价格，如有产品需要干冰运输，需另外加收干冰运输费。 |