1. Metabolic Enzyme/Protease
    Apoptosis
  2. Phospholipase
    Lipoxygenase
    Ferroptosis
  3. U-73122

U-73122 

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

U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC.

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

U-73122 Chemical Structure

U-73122 Chemical Structure

CAS No. : 112648-68-7

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 90 In-stock
Estimated Time of Arrival: December 31
50 mg USD 300 In-stock
Estimated Time of Arrival: December 31
100 mg USD 550 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 31 publication(s) in Google Scholar

Top Publications Citing Use of Products

    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: 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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50of 1-2.1 µM for PLC.

    IC50 & Target

    5-LOX

     

    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].

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

    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].

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

    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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 12.5 mg/mL (26.90 mM; Need ultrasonic)

    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.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 1.25 mg/mL (2.69 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 1.25 mg/mL (2.69 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 1.25 mg/mL (2.69 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    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

    Purity: 98.17%

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    Keywords:

    U-73122U73122U 73122PhospholipaseLipoxygenaseFerroptosisLOXInhibitorinhibitorinhibit

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