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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
smooth muscle cells 2 µM U-73122 blocks Ca2+ release by inhibiting the SERCA pump Br J Pharmacol. 2010 Jul;160(6):1293-4.
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. Mol Cancer. 2010 Jun 21;9:156.
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. Plant Cell. 2006 Dec;18(12):3519-34.
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. Proc Natl Acad Sci U S A. 1999 Feb 16;96(4):1779-84.
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. Proc Natl Acad Sci U S A. 1999 Feb 16;96(4):1779-84.
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. Proc Natl Acad Sci U S A. 2013 Jul 2;110(27):11181-6.
COS7 cells 1 µM Block PLC, abolish M1 receptor-mediated inhibition of KATP current Proc Natl Acad Sci U S A. 1999 Dec 21;96(26):15292-7.
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. J Neuroinflammation. 2014 Nov 19;11:190.
BV-2 microglia 5 μM 1 hour U-73122 completely abolished the MPEP-induced increase in Ca2+ and prevented the MPEP-dependent induction of CHOP, GRP78, and GRP96 mRNA expression. J Neuroinflammation. 2014 Nov 19;11:190.
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. Br J Pharmacol. 2010 Jul;160(6):1295-301.
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. Br J Pharmacol. 2010 Jul;160(6):1295-301.
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. Br J Pharmacol. 2010 Jul;160(6):1295-301.
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. Br J Pharmacol. 1995 May;115(1):11-4.

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. Br J Pharmacol. 2018 Sep;175(18):3727-3737

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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