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U-73122
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
U-73122图片
CAS NO:112648-68-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议

产品介绍

化学性质

Physical AppearanceA solid
StorageStore at -20°C
M.Wt464.64
Cas No.112648-68-7
FormulaC29H40N2O3
Solubilityinsoluble in H2O; ≥15.5 mg/mL in EtOH with gentle warming and ultrasonic; ≥5.67 mg/mL in DMSO with gentle warming
Chemical Name1-[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
Canonical SMILESCC12CCC3C(C1CCC2NCCCCCCN4C(=O)C=CC4=O)CCC5=C3C=CC(=C5)OC
运输条件蓝冰运输或根据您的需求运输。
一般建议为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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.

试验操作

Cell experiment:[1]

Cell lines

Human neutrophils

Reaction Conditions

15 min or 3 h incubation

Applications

In human neutrophils, U-73122 reduced interleukin-8 and leukotriene B4-induced Ca2+flux (after 15 min incubation) and chemotaxis (after 3 h incubation) in a concentration-dependent manner, with IC50 values being ~6 μM and ~5 μM, respectively.

Animal experiment:[1]

Animal models

Male Sprague-Dawley rats, ~ 200 g

Dosage form

30 mg/kg

Administered intraperitoneally (i.p.)

Applications

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. U-73122 significantly inhibited carrageenan-induced inflammation, and its effect was more complete than a 10 mg/kg p.o. dose of indomethacin.

Note

The technical data provided above is for reference only.

References:

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.