U-73122 CAS号: 112648-68-7分子式: C29H40N2O3分子量: 464.64描述纯度储存/保存方法别名外观可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC. |
纯度 |
98%
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储存/保存方法 |
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
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基本信息 | |
别名 |
U73122;U 73122
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外观 |
off-white solid
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可溶性/溶解性 |
DMSO : 12.5 mg/mL (26.90 mM; Need ultrasonic)
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生物活性 | |
靶点 |
5-LOX
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In vitro(体外研究) |
U-73122 potently inhibits receptor-coupled activation of PLC in membranes isolated from PMNs. U-73122 inhibits N-formyl-methionyl-leucyl-phenylalanine-induced aggregation of human polymorphonuclear neutrophils (PMN) and the associated production of IP3 and diacyglycerol. U-73122 markedly inhibits inositol phosphate release elicited by either oxotremorine-M or guanosine-5′-O-(3-thiotriphosphate) than that induced by added Ca2+ in digitonin-permeabilized cells.
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In vivo(体内研究) |
U73122 significantly attenuates TNF-α mRNA expression, has no effect on sham animals, but significantly increases heart work and rate of contraction and relaxation without affecting heart rate in endotoxemic mice. U73122 (400 nM/μL) significantly reduces total lordosis durations, compared to vehicle infusions to the VTA, of oestradiol and progesterone-primed hamsters. VTA infusions of U73122 do not alter motor behaviour of hamsters in the activity monitor, but there is a significant effect of muscimol to decrease total number of beam breaks compared to hamsters administered SKF38393.
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分子结构图