MRS 2578
- MRS-2578；MRS2578
货号： abs813735
| 货号-规格 | 货期 | 价格 | 数量 |
| abs813735-10mg | 1-2周 | ￥582.00 | - + |
| abs813735-25mg | 1-2周 | ￥1237.00 | - + |
| abs813735-50mg | 1-2周 | ￥2098.00 | - + |
| abs813735-100mg | 1-2周 | ￥3776.00 | - + |
大包装询价| 产品描述 | ||
| 描述 | MRS 2578是一种有效的P2Y6受体抑制剂，IC50为37 nM，对P2Y1， P2Y2， P2Y4和P2Y11受体的作用活性很弱。MRS2578 选择性阻断P2Y6受体活性，而不影响P2Y1, P2Y2, P2Y4或P2Y11 受体。在1321N1星形细胞瘤细胞中MRS2578 (1 μM) 可以完全阻断UDP对TNFalpha诱导的细胞凋亡的保护作用。 在转染有0.25 μg NF-κB启动子报告基因的HMEC-1细胞中，MRS 2578抑制 本底的NF-κB 活性并具有时间和剂量依赖特性。 | |
| 纯度 | >98% | |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. | |
| 基本信息 | ||
| 别名 | MRS-2578；MRS2578 | |
| 外观 | 白色粉末 | |
| 可溶性/溶解性 | DMSO ：23.6 mg/mL (50 mM) | |
| 生物活性 | ||
| 靶点 | P2Y6 | |
| In vitro(体外研究) | MRS2578 selectively blocks P2Y6 receptor activity versus activity at P2Y1, P2Y2, P2Y4 or P2Y11 receptors. MRS2578 (1 μM) completely blocks the protection by UDP undergoing TNFalpha-induced apoptosis in 1321N1 astrocytoma cells. MRS 2578 inhibits basal NF-κB activity in time and dose dependent manner in HMEC-1 cells transfected with 0.25 μg NF-κB promoter reporter. MRS 2578 (10 μM) completely abolishes TNF-α induced NF-κB reporter activity in HMEC-1 cells. MRS 2578 (10 μM) significant reduces TNF-α–induced proinflammatory gene expression in HMEC-1 cells. MRS 2578 potentiates ATPγS and UDP response at concentrations below 316 nM whereas above this concentration, MRS 2578 inhibits ATPS- and UDP-induced IP accumulation in neonatal rat cardiac myofibroblasts. MRS2578-treated mice shows reduced bronchial hyperresponsiveness toward methacholine in OVA-sensitized mice. MRS2578 completely blocks UDP-induced the release of IL-6, KC, and IL-8 in lung epithelial cells. | |
| In vivo(体内研究) | MRS 2578 (10 μM) attenuates Keratinocyte-derived chemokine serum protein levels in LPS-induced vascular inflammation in C57BL/6 mice. MRS2578 (10 μM, intratracheally) reduces BALF eosinophilia and the levels of IL-5 and IL-13 in the BALF in OVA-sensitized mice and leads to a markedly attenuated change in methacholine responsiveness after OVA challenge. MRS2578 (10 μM, intratracheally) inhibits house dust mite–induced allergic airway inflammation in OVA-sensitized mice. MRS2578 (10 μM, intratracheally) reduces of IL-6 and KC levels in BALF in OVA-sensitized mice. | |
| 温馨提示：本产品仅作科研实验使用，不支持临床等研究 |
- 实验方法 实验条件
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