U-73122
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in DMSO) | ￥909.00 | 现货 | |
| 5mg | ￥581.00 | 现货 | |
| 10mg | ￥872.00 | 现货 | |
| 25mg | ￥1636.00 | 现货 |
特色产品
- 适用于流式细胞仪和荧光显微镜检测
- 准确区分活细胞/凋亡细胞/坏死细胞
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 对细胞无毒性
- 步骤更简单，无需有机溶剂
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
- 优异的扩增效率、可重复性和稳定性
- 卓越的灵敏度和准确性，操作简单
- 优化的缓冲液和T7 RNA聚合酶混合物
- 20 μL反应体系可获得更高的RNA产量
产品描述
U-73122 is a potent phospholipase C (PLC) inhibitor with IC50 value of ~6 μM [1].
PLC is a class of membrane-associated enzymes that catalyzes the hydrolysis of a membrane phospholipid, phosphatidylinositol 4,5-bisphosphate (PIP2), to produce two intracellular messengers, diacylglycerol and inositol-triphosphate, which, in turn, mediate the activation of protein kinase C (PKC) and intracellular Ca2+ release, respectively. It plays an important role in various signal transduction pathways [1].
U-73122 significantly inhibited recombinant human PLC-β2 with IC50 value of ~6 μM, while showing little effect on PLC-β1, PLC-β3 or PLC-β4. In human neutrophils, U-73122 reduced interleukin-8 and leukotriene B4-induced Ca2+ flux and chemotaxis with IC50 values of ~6 μM and ~5 μM, respectively [1].
In rats, U-73122 (30 mg/kg, i.p.) inhibited hind paw swelling by 65% and 80% at 1 h and 3 h post-carrageenan challenge. Moreover, pretreatment of U-73122 (1 mg/kg, 3 mg/kg and 10 mg/kg, respectively, i.v.) effectively suppressed TPA-induced mouse ear edema in a dose-dependent manner [1].
Reference:
[1]. Hou C, Kirchner T, Singer M, et al. In vivo activity of a phospholipase C inhibitor, 1-(6-((17beta-3-methoxyestra-1,3,5(10)-trien-17-yl)amino)hexyl)-1H-pyrrole-2,5-dione (U73122), in acute and chronic inflammatory reactions. Journal of Pharmacology and Experimental Therapeutics, 2004, 309(2): 697-704.
产品性质
| 物理外观 | A solid |
| CAS号 | 112648-68-7 |
| 分子式 | C29H40N2O3 |
| 分子量 | 464.64 |
| 化学名称 | 1-[6-[[(8R,9S,13S,14S,17S)-3-methoxy-13-methyl-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthren-17-yl]amino]hexyl]pyrrole-2,5-dione |
| 溶解度 | insoluble in H2O; ≥15.5 mg/mL in EtOH with gentle warming and ultrasonic; ≥5.67 mg/mL in DMSO with gentle warming |
| SMILES | C[C@](CC1)([C@@H](CC2)[C@H](CC3)[C@H]1c(cc1)c3cc1OC)[C@H]2NCCCCCCN(C(C=C1)=O)C1=O |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献，APExBIO并未验证，仅供参考)
IC50和靶点
| 生物活性描述 | U-73122 是一种磷脂酶 C（PLC）和 5-LO（5-脂氧合酶）抑制剂，PLC 的 IC50 为 1-2.1 μM。 |
生物相关数据
质量控制
操作说明
APExBIO 顾客使用本产品发表的 1 篇科研文献
- 1. Chien-Liang Liu, Shih-Ping Cheng, et al. "Quinolinate Phosphoribosyltransferase Promotes Invasiveness of Breast Cancer Through Myosin Light Chain Phosphorylation." Front Endocrinol (Lausanne). 2021 Feb 4;11:621944. PMID: 33613454 2. Zhou J, Lai W, et al. "BLT1 in dendritic cells promotes Th1/Th17 differentiation and its deficiency ameliorates TNBS-induced colitis." Cell Mol Immunol. 2018 Apr 18. PMID:29670278
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