U-73122
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 464.64 |
| Cas No. | 112648-68-7 |
| Formula | C29H40N2O3 |
| Solubility | insoluble in H2O; ≥15.5 mg/mL in EtOH with gentle warming and ultrasonic; ≥5.67 mg/mL in DMSO with gentle warming |
| Chemical Name | 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 |
| SDF | Download SDF |
| Canonical SMILES | CC12CCC3C(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 | 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。 |
| Cell experiment:[1] | |
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Cell lines |
Human neutrophils |
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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] | |
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Animal models |
Male Sprague-Dawley rats, ~ 200 g |
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Dosage form |
30 mg/kg Administered intraperitoneally (i.p.) |
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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. |
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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. |
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质量控制和MSDS
- 批次:
化学结构
相关生物数据
