Powder: -20°C for 3 years | In solvent: -80°C for 1 year
U-73122 (U73122) 是一种磷脂酶 C 和 5-脂氧合酶抑制剂,对磷脂酶 C 的 IC50值约为 1-2.1 µM。它是一种 PLC 抑制剂,可减少激动剂诱导的血小板和 PMN 中的 Ca2+ 增加。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 297 | 现货 | ||
5 mg | ¥ 473 | 现货 | ||
10 mg | ¥ 738 | 现货 | ||
25 mg | ¥ 1,380 | 现货 | ||
50 mg | ¥ 2,490 | 现货 | ||
100 mg | ¥ 3,770 | 现货 | ||
500 mg | ¥ 8,380 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 547 | 现货 |
产品描述 | U-73122 (U73122) , an effective PLC inhibitor, reduces agonist-induced Ca2+ increases in platelets and PMN. |
体外活性 | 0.1 mg/ml U73122分别抑制狗体内角叉菜胶诱导的74%淋巴细胞和65%巨噬细胞积累到皮下腔隙.30 mg/kg U73122(i.p.)阻断角叉菜胶处理1小时和3小时后大鼠后爪65%和80%的水肿.其还完全抑制小鼠腹膜炎模型中脂多糖诱导的巨噬细胞和淋巴细胞浸润,以及前列腺素E2(80%),并且也会抑制12-O-十四酰-佛波醇-13-乙酸盐诱导的小鼠耳肿胀. |
体内活性 | U-73122抑制胶原蛋白诱导的血栓素B的产生,胶原蛋白通过抑制受体耦合的花生四烯酸转移产生诱导作用。U73122也会抑制FMLP诱导的人多形核中性白细胞聚合,以及相关的IP3和甘油二酯的产生。U73122明显抑制各种激动剂,包括凝血酶,胶原蛋白,ADP,花生四烯酸诱导的人血小板的聚集(IC50为1-5 μM)。凝血酶或者U-46619通过抑制被血小板可溶组分催化的磷脂酰[3H]肌糖和磷脂酰[3H]肌糖4,5-二磷酸的水解(Ki:9/40 μM),诱导IP3的产生和随后细胞溶质中Ca2+的快速增加,10 μM U-73122会对其产生抑制。 |
激酶实验 | PMNs (4×107/4 mL) are incubated with U-73122 according to protocols. The reactions are stopped with cold calcium-free PBS. The cells are centrifuged at 750 × g (4°C) and resuspended in 1 mL of Triton X-100-free extraction buffer (50 mM Tris, pH 7.5, 50 mM fimercaptoethanol, 2 mM EGTA, 1 mM phenylmethylsulfonyl fluoride and 4 μg/mL of leupeptin, soybean trypsin inhibitor and aprotinin), and then sonicated for 10- and 5-sec consecutive bursts at 20% output. The lysates are centrifuged at 240 × g (4°C) for 20 mm in a TL-100 ultracentrifuge with the supernatant designated as the cytosol fraction. The pellet is resuspended in 1% Triton-containing extraction buffer, sonicated, shaken for 30 mm at 4°C and centrifuged (240 × g for 20 mm at 4°C). The supernatant constitutes the extractable particulate fraction, and the pellet is sonicated in extraction buffer with Triton and constituted the nonextractable particulate fraction. |
细胞实验 | U-73122 is dissolved in DMSO. Agonist-induced production of IP3 in PMN is measured by use of the competitive radiobinding assy. PMN (2 x 106-107) in 0.2 mL of phosphate-buffered saline, pH 7.4 [NaC1 (138 mM), Na2HPO4 (8.1 mM), KH2PO4 (1.5 mM), KCI (2.7 mM), CaCl2 (1.0 mM), MgC12 (1.0 mM) and glucose (0.1%, w/v)] are incubated in conical polypropylene tubes at 37°C in a shaking water bath. U-73122 or U-73343 is added (in 1 μL of DMSO) 3 min before the addition of agonist, FMLP (0.1 μM) plus cytochalasin B (5 μg/mL). FMLP and cytochalasin B are added in 1 μL each of DMSO and ethanol, respectively. Appropriate vehicle controls are included in each experiment. PMN incubation mixtures are quenched with the addition of 0.07 mL of ice-cold TCA (20%, w/v) and a portion (0.2 mL) of the TCA extract is processed for the measurement of IP3 by competitive radiobinding as described above for platelets. |
别名 | U73122 |
分子量 | 464.64 |
分子式 | C29H40N2O3 |
CAS No. | 112648-68-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 12.5 mg/mL (26.90 mM), Sonication is recommended.
H2O: < 0.1 mg/mL (insoluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1522 mL | 10.761 mL | 21.522 mL | 53.8051 mL |
5 mM | 0.4304 mL | 2.1522 mL | 4.3044 mL | 10.761 mL | |
10 mM | 0.2152 mL | 1.0761 mL | 2.1522 mL | 5.3805 mL | |
20 mM | 0.1076 mL | 0.5381 mL | 1.0761 mL | 2.6903 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
U-73122 112648-68-7 Apoptosis Metabolism Ferroptosis Phospholipase Lipoxygenase inhibit Inhibitor U73122 U 73122 LOX inhibitor