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网站主页 化工产品目录 生物化工 抑制剂 代谢(Metabolism) Phospholipase (e.g. PLA) 抑制剂 1-[6-[((17Β)-3-雌酮-1,3,5[10]-三烯-17-基)氨基]乙基]-1H-吡咯-2,5-二酮 化合物 U73122
  • 化合物 U73122|T6243|TargetMol

化合物 U73122|T6243|TargetMol

U-73122
112648-68-7
297 2mg 起订
473 5mg 起订
738 10mg 起订
上海 更新日期:2024-12-02

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产品详情:

中文名称:
化合物 U73122
英文名称:
U-73122
CAS号:
112648-68-7
品牌:
TargetMol
产地:
美国
保存条件:
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
纯度规格:
96.73%
产品类别:
抑制剂
货号:
T6243

Product Introduction

Bioactivity

名称U-73122
描述U-73122 (U73122) , an effective PLC inhibitor, reduces agonist-induced Ca2+ increases in platelets and PMN.
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.
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.
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。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度DMSO : 5.63 mg/mL (12.11 mM), Sonication is recommended.
H2O : < 0.1 mg/mL (insoluble)
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1.25 mg/mL (2.69 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
关键字inhibit | Phospholipase | Inhibitor | U-73122 | Ferroptosis | Lipoxygenase | U 73122 | LOX
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U73122|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。

成立日期 (12年)
注册资本 589.8595万人民币
员工人数 100-500人
年营业额 ¥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 中间体,天然产物,生物化工,化学试剂,生物技术服务

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