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Chemical Structure| 112648-68-7 Chemical Structure| 112648-68-7

Structure of U-73122
CAS No.: 112648-68-7

Chemical Structure| 112648-68-7

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U-73122 is an inhibitor of phospholipase C, phospholipase A2, and 5-LO(5-lipoxygenase).

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Product Details of U-73122

CAS No. :112648-68-7
Formula : C29H40N2O3
M.W : 464.64
SMILES Code : O=C(C=C1)N(CCCCCCN[C@H]2CC[C@@]3([H])[C@]4([H])CCC5=CC(OC)=CC=C5[C@@]4([H])CC[C@]23C)C1=O
MDL No. :MFCD00893825
InChI Key :LUFAORPFSVMJIW-ZRJUGLEFSA-N
Pubchem ID :104794

Safety of U-73122

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
COS7 cells 1 µM Block PLC, abolish M1 receptor-mediated inhibition of KATP current PMC24813
Smooth muscle cells 2 µM U-73122 blocks Ca2+ release by inhibiting the SERCA pump PMC2938801
MCF-7 cells 20 μM U-73122 was able to prevent intracellular Ca2+ elevation in response to serum, whereas the inactive analogue U-73343 was ineffective. PMC2906470
Tobacco pollen tubes 80 µM 20 min U-73122 inhibited the PI 4,5-P2 hydrolyzing activity of Nt PLC3, with complete inhibition at 80 µM. PMC1785407
Recombinant plant PI-PLC 0-120 µM 15 min U-73122 inhibited the hydrolytic activity of recombinant plant PI-PLC in a dose-dependent manner, with an IC50 of 23 µM. PMC15593
Guard cells 1 µM 15 min Inhibited ABA-induced oscillations in cytosolic free calcium and stomatal closure, but did not inhibit external calcium-induced oscillations and stomatal closure. PMC15593
Purkinje cells 5 μM To study the effect of U-73122 on PF-LTP, it was found that U-73122 rescued PF-LTP, indicating that mAChR-dependent cannabinoid production relies on PLC. PMC3704018
BV-2 microglia 5 μM 2 h U-73122 significantly reduced the MPEP-induced increase in total PLC activity and decreased the MPEP-induced up-regulation of GRP78 protein expression. PMC4240888
BV-2 microglia 5 μM 1 h U-73122 completely abolished the MPEP-induced increase in Ca2+ and prevented the MPEP-dependent induction of CHOP, GRP78, and GRP96 mRNA expression. PMC4240888
Colonic smooth muscle cells 10 µM U-73122 inhibited caffeine-evoked [Ca2+]cyto increases, suggesting it may reduce Ca2+ release by inhibiting the SR Ca2+ pump. PMC2938802
Colonic smooth muscle cells 1 µM U-73122 inhibited [Ca2+]cyto increases evoked by photolysis of caged IP3, suggesting it may reduce Ca2+ release by inhibiting the SR Ca2+ pump. PMC2938802
Colonic smooth muscle cells 10 µM U-73122 inhibited carbachol-evoked [Ca2+]cyto increases, suggesting it may reduce IP3 generation by inhibiting PI-PLC activity. PMC2938802
Mouse L fibroblasts (L cells) 0-6 μM U-73122 inhibited ATP and LPA-induced Ca2+ transients in a dose-dependent manner, with EC50 values of 1.5 μM and 3.5 μM, respectively. PMC1908738

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Urodynamic model Intracerebroventricular injection 300 or 1000 pmol/rat Single administration, observed for 60 minutes Pretreatment with U-73122 significantly suppressed central Ang II-induced shortening of the intercontraction interval, indicating the role of PLC in Ang II-induced frequent urination. PMC6109218

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.15mL

0.43mL

0.22mL

10.76mL

2.15mL

1.08mL

21.52mL

4.30mL

2.15mL

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