1. Metabolic Enzyme/Protease
  2. 5-Lipoxygenase
    Phospholipase

U-73122 

Cat. No.: HY-13419 Purity: 98.17%
Handling Instructions

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

For research use only. We do not sell to patients.

U-73122 Chemical Structure

U-73122 Chemical Structure

CAS No. : 112648-68-7

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
5 mg USD 77 In-stock
Estimated Time of Arrival: December 31
10 mg USD 115 In-stock
Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

    U-73122 purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    MCF-7 cells are pretreated with the indicated chemical inhibitors for 30min, followed by 15 min treatment with RA (20 μM) + EPA (80 μM).Cell extracts are prepared and subjected to western blotting analysis.

    U-73122 purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    Cell morphology of MCF-7 treated with RA (20 μM)+ω-3 PUFAs (80 μM) with or without 3-MA (5 mM) for 24h.

    U-73122 purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 22;8(65):109135-109150.

    Cells are treated with RA (20 μM) plus ω-3 PUFAs (80 μM) with or without CQ (5 μM) for 24 h. Cell extracts are prepared and subjected to western blotting analysis.

    U-73122 purchased from MCE. Usage Cited in: J Mol Neurosci. 2015 Aug;56(4):848-57.

    Effect of LXA4 on astrocyte viability. Cell viability is measured by MTT reduction assay. Results are expressed as the percentage of MTT reduction normalized to the control group (100 %). The MTT reduction is reduced by OGDR, but is significantly increased by LXA4. The effect is not antagonized by Boc2, but partly reversed by U73122 and T0070907.

    U-73122 purchased from MCE. Usage Cited in: J Mol Neurosci. 2015 Aug;56(4):848-57.

    a Statistical analysis showing the prevention effect of minocycline pretreatment (40 mg/kg/day) on CUS-, CRS- or CSDS-induced decreases in hippocampal microglial numbers. b, c Statistical analysis showing the prevention effect of minocycline pretreatment (40 mg/kg/day) on CUS-, CRS- or CSDS-induced increases in the immobile time in the TST (b) and FST (c). d, e Statistical analysis showing the prevention effect of minocycline pretreatment (40 mg/kg/day) on CUS-, CRS- or CSDS-induced decreases in
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    In Vitro

    U-73122 potently inhibits receptor-coupled activation of PLC in membranes isolated from PMNs[1]. U-73122 inhibits N-formyl-methionyl-leucyl-phenylalanine-induced aggregation of human polymorphonuclear neutrophils (PMN) and the associated production of IP3 and diacyglycerol[2]. 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[3].

    In Vivo

    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[4]. 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[5].

    Solvent & Solubility
    In Vitro: 

    10 mM in DMSO

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1522 mL 10.7610 mL 21.5220 mL
    5 mM 0.4304 mL 2.1522 mL 4.3044 mL
    10 mM 0.2152 mL 1.0761 mL 2.1522 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    PMNs (4×107/4 mL) are incubated with U-73122 according to protocols. The reactions are stopped with cold calcium-free PBS. The cells are centrifuged at 750 × g (4°C) and resuspended in 1 mL of Triton X-100-free extraction buffer (50 mM Tris, pH 7.5, 50 mM fimercaptoethanol, 2 mM EGTA, 1 mM phenylmethylsulfonyl fluoride and 4 μg/mL of leupeptin, soybean trypsin inhibitor and aprotinin), and then sonicated for 10- and 5-sec consecutive bursts at 20% output. The lysates are centrifuged at 240 × g (4°C) for 20 mm in a TL-100 ultracentrifuge with the supernatant designated as the cytosol fraction. The pellet is resuspended in 1% Triton-containing extraction buffer, sonicated, shaken for 30 mm at 4°C and centrifuged (240 × g for 20 mm at 4°C). The supernatant constitutes the extractable particulate fraction, and the pellet is sonicated in extraction buffer with Triton and constituted the nonextractable particulate fraction.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [2]

    Agonist-induced production of IP3 in PMN is measured by use of the competitive radiobinding assy. PMN (2 x 106-107) in 0.2 mL of phosphate-buffered saline, pH 7.4 [NaC1 (138 mM), Na2HPO4 (8.1 mM), KH2PO4 (1.5 mM), KCI (2.7 mM), CaCl2 (1.0 mM), MgC12 (1.0 mM) and glucose (0.1%, w/v)] are incubated in conical polypropylene tubes at 37°C in a shaking water bath. U-73122 or U-73343 is added (in 1 μL of DMSO) 3 min before the addition of agonist, FMLP (0.1 μM) plus cytochalasin B (5 μg/mL). FMLP and cytochalasin B are added in 1 μL each of DMSO and ethanol, respectively. Appropriate vehicle controls are included in each experiment. PMN incubation mixtures are quenched with the addition of 0.07 mL of ice-cold TCA (20%, w/v) and a portion (0.2 mL) of the TCA extract is processed for the measurement of IP3 by competitive radiobinding as described above for platelets.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [5]

    Hamsters are hormone-primed with 17β-oestradiol at h 0 and progesterone at h 45. At h 48, hamsters are pretested for motor behaviour, followed by sexual behaviour testing, and bilateral infusions of U73122 (400 nM/µL) or saline vehicle. Thirty minutes after infusions, hamsters are re-tested for sexual behaviour (post inhibitor infusion test) and, immediately after testing, infused bilaterally with SKF38393 (100 ng/µL), muscimol (100 ng/µL), or saline vehicle. Thirty minutes after the agonist or vehicle infusions, lordosis and motor behaviour of hamsters is reassessed (post agonist infusion test). All hamsters are assigned to one pretreatment condition, U73122 or vehicle, and are tested once a week for 3 weeks until all infusion conditions (SKF38393, muscimol or vehicle), are received. The order in which hamsters receive SKF38393, muscimol or vehicle infusions is counterbalanced across the group. 

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    464.64

    Formula

    C₂₉H₄₀N₂O₃

    CAS No.

    112648-68-7

    SMILES

    O=C(C=C1)N(CCCCCCN[[email protected]]2CC[[email protected]@]3([H])[[email protected]]4([H])CCC5=C(C=CC(OC)=C5)[[email protected]@]4([H])CC[[email protected]]23C)C1=O

    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

    Purity: 98.17%

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product name

     

    Salutation

    Applicant name *

     

    Email address *

    Phone number *

     

    Organization name *

    Country or Region *

     

    Requested quantity *

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    U-73122
    Cat. No.:
    HY-13419
    Quantity:

    U-73122

    Cat. No.: HY-13419