2. GPCR/G Protein
  3. Protease Activated Receptor (PAR)
  4. AZ3451

AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.

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

CAS No. : 2100284-59-9

Size Price Stock Quantity
Free Sample (0.1 - 0.2 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

AZ3451 Related Antibodies

Top Publications Citing Use of Products

    AZ3451 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2019 Dec 16;11(24):12532-12545.  [Abstract]

    AZ3451 (0-20 μM) can effectively inhibit PAR2 expression in chondrocytes.

    AZ3451 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2019 Dec 16;11(24):12532-12545.  [Abstract]

    AZ3451 (0-20 μM) can effectively inhibit PAR2 expression in chondrocytes.

    AZ3451 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2019 Dec 16;11(24):12532-12545.  [Abstract]

    IL-1β increased the inflammatory cytokines and catabolic genes expression, including iNOS, COX2, MMP1, MMP13 and ADAMTS5, while treatment with AZ3451 (10 μM) alleviated this process.

    AZ3451 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2019 Dec 16;11(24):12532-12545.  [Abstract]

    The IL-1β-treated chondrocytes exerted higher SA-β-gal activity and p16INK4a protein expression compared with the control group, while PAR2 antagonist AZ3451 (10 μM) significantly prevented this process.

    AZ3451 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2019 Dec 16;11(24):12532-12545.  [Abstract]

    After infection with the GFP-RFP-LC3 adenovirus, there was fewer red puncta under IL-1β stimulation in chondrocytes; However, AZ3451 treatment cells presented more red puncta. These results demonstrated that AZ3451 could enhance autophagosome conversion to autophagolysosomes and thus promoting autophagy flux and autophagy level.

    AZ3451 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2019 Dec 16;11(24):12532-12545.  [Abstract]

    AZ3451 treatment downregulated the IL-1β-induced increasing levels of TUNEL positive cells.

    AZ3451 purchased from MedChemExpress. Usage Cited in: Aging (Albany NY). 2019 Dec 16;11(24):12532-12545.  [Abstract]

    AZ3451 treatment caused a marked decrease of apoptotic chondrocytes induced by IL-1β.

    View All Protease Activated Receptor (PAR) Isoform Specific Products:

    View All Isoforms
    PAR1 PAR2 PAR4

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    AZ3451 is a potent protease-activated receptor-2 (PAR2) antagonist with IC50 of 23 nM.

    IC50 & Target

    PAR2

    23 nM (IC50)

    In Vitro

    Antagonist AZ3451 binds to a remote allosteric site outside the helical bundle of the protease-activated receptor 2. AZ3451 is highly lipophilic, which coincides with the hydrophobic nature of the binding pocket within the membrane. Antagonist binding prevents structural rearrangements required for receptor activation and signalling[1].

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

    AZ3451 Related Antibodies
    Molecular Weight

    571.46

    Formula

    C30H27BrN4O3
    CAS No.
    Appearance

    Solid

    Color

    White to light brown

    SMILES

    O=C(C1=CC=C2C(N=C(C3=C(Br)C=C(OCO4)C4=C3)N2[C@H](C5CCCCC5)C)=C1)NC6=CC=C(C#N)C=C6
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (174.99 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7499 mL 8.7495 mL 17.4990 mL
    5 mM 0.3500 mL 1.7499 mL 3.4998 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

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

      Solubility: ≥ 2.08 mg/mL (3.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.64 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.84%

    SDS (393 KB)

    COA (250 KB) HNMR (301 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7499 mL 8.7495 mL 17.4990 mL 43.7476 mL
    5 mM 0.3500 mL 1.7499 mL 3.4998 mL 8.7495 mL
    10 mM 0.1750 mL 0.8750 mL 1.7499 mL 4.3748 mL
    15 mM 0.1167 mL 0.5833 mL 1.1666 mL 2.9165 mL
    20 mM 0.0875 mL 0.4375 mL 0.8750 mL 2.1874 mL
    25 mM 0.0700 mL 0.3500 mL 0.7000 mL 1.7499 mL
    30 mM 0.0583 mL 0.2917 mL 0.5833 mL 1.4583 mL
    40 mM 0.0437 mL 0.2187 mL 0.4375 mL 1.0937 mL
    50 mM 0.0350 mL 0.1750 mL 0.3500 mL 0.8750 mL
    60 mM 0.0292 mL 0.1458 mL 0.2917 mL 0.7291 mL
    80 mM 0.0219 mL 0.1094 mL 0.2187 mL 0.5468 mL
    100 mM 0.0175 mL 0.0875 mL 0.1750 mL 0.4375 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    AZ3451 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    AZ34512100284-59-9AZ 3451AZ-3451Protease Activated Receptor (PAR)Thrombin receptorsInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    AZ3451
    Cat. No.:
    HY-112558
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.