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U-73122
Cat. No. IC23031
CAS. No. 112648-68-7
Key Features and Details
Category
Inhibitor&Activator
Purity
≥98.0%
Formula
C29H40N2O3
Product Details
Product Name
U-73122
CAS No.
112648-68-7
Molecular Weight
464.64
Target
5-LOX
Formula
C29H40N2O3
Appearance
Solid
Purity
≥98.0%
SMILES
O=C(C=C1)N(CCCCCCN[C@H]2CC[C@@]3([H])[C@]4([H])CCC5=C(C=CC(OC)=C5)[C@@]4([H])CC[C@]23C)C1=O
Product Overview
Description
U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC.
In Vitro Activity
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.
In Vivo Activity
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.
Storage & Handling
Storage
Powder, -20 °C, 3 years; 4 °C, 2 years
In solvent: -80 °C, 6 months, -20 °C, 1 month.
Shipping
Room temperature in continental US; may vary elsewhere.
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