1. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Autophagy
  2. PPAR Autophagy
  3. GW 501516

GW 501516  (Synonyms: GW 1516; GSK-516)

Cat. No.: HY-10838 Purity: 99.43%
SDS COA Handling Instructions

GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM.

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

GW 501516 Chemical Structure

GW 501516 Chemical Structure

CAS No. : 317318-70-0

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Customer Review

Based on 16 publication(s) in Google Scholar

Other Forms of GW 501516:

Top Publications Citing Use of Products

    GW 501516 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 28;9:648.  [Abstract]

    Western blot analysis of the protein expression of caspase and Bcl-2 family members in response to GW501516.

    View All PPAR Isoform Specific Products:

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    GW 501516 (GW 1516) is a PPARδ agonist with an EC50 of 1.1 nM[1].

    IC50 & Target[1]

    PPARδ

    1.1 nM (EC50)

    Cellular Effect
    Cell Line Type Value Description References
    COS-1 EC50
    > 1000 nM
    Compound: 1, GW-501516
    Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay
    Agonist activity at human PPARalpha ligand binding domain expressed in COS-1 cells co-transfected with Gal4 after 24 hrs by luciferase reporter gene assay
    [PMID: 22051054]
    COS-1 EC50
    0.5 nM
    Compound: 1, GW501516
    Agonist activity at pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay
    Agonist activity at pSG5-Gal4-tagged human PPAR-beta/delta ligand binding domain expressed in COS1 cells assessed as receptor activation incubated for 19 hrs by pGL3-5XUAS-SV40 luciferase reporter gene assay
    [PMID: 25768705]
    COS-1 EC50
    2.9 nM
    Compound: 1, GW-501516
    Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
    Agonist activity at human PPARdelta ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
    [PMID: 22051054]
    COS-1 EC50
    912 nM
    Compound: 1, GW-501516
    Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
    Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells after 24 hrs by luciferase reporter gene-based luminometric analysis
    [PMID: 22051054]
    COS-7 EC50
    1 nM
    Compound: GW-501516
    Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells
    Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells
    [PMID: 16797985]
    COS-7 EC50
    10000 nM
    Compound: GW-501516
    Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells
    Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells
    [PMID: 16797985]
    COS-7 EC50
    10000 nM
    Compound: GW-501516
    Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells
    Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells
    [PMID: 16797985]
    CV-1 EC50
    > 1.2 μM
    Compound: GW501516
    Transactivation activity at human PPARgamma expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Transactivation activity at human PPARgamma expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22534184]
    CV-1 EC50
    0.001 μM
    Compound: 1, GW-501516
    Agonist potency at PPARdelta in CV1 cells by cell based transient transfection assay
    Agonist potency at PPARdelta in CV1 cells by cell based transient transfection assay
    [PMID: 17243659]
    CV-1 EC50
    0.0012 μM
    Compound: GW501516
    Transactivation of human PPARdelta expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of human PPARdelta expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 22579420]
    CV-1 EC50
    0.0017 μM
    Compound: 1, GW-501516
    Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    [PMID: 21515063]
    CV-1 EC50
    0.0017 μM
    Compound: GW-501516
    Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of Gal4-fused human PPARdelta DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 21112784]
    CV-1 EC50
    0.99 μM
    Compound: 1, GW-501516
    Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    [PMID: 21515063]
    CV-1 EC50
    0.99 μM
    Compound: GW-501516
    Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of Gal4-fused human PPARalpha DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 21112784]
    CV-1 EC50
    1.888 μM
    Compound: 1, GW-501516
    Agonist potency at PPARalpha in CV1 cells by cell based transient transfection assay
    Agonist potency at PPARalpha in CV1 cells by cell based transient transfection assay
    [PMID: 17243659]
    CV-1 EC50
    2.5 nM
    Compound: GW501516
    Transactivation activity at human PPARdelta expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Transactivation activity at human PPARdelta expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22534184]
    CV-1 EC50
    229 nM
    Compound: GW501516
    Transactivation activity at human PPARalpha expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    Transactivation activity at human PPARalpha expressed in african green monkey CV1 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 22534184]
    CV-1 EC50
    4.1 μM
    Compound: 1, GW-501516
    Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
    [PMID: 21515063]
    CV-1 EC50
    4.1 μM
    Compound: GW-501516
    Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    Transactivation of Gal4-fused human PPARgamma DNA binding domain expressed in african green monkey CV1 cells by luciferase reporter gene assay
    [PMID: 21112784]
    CV-1 EC50
    8.9 μM
    Compound: 1, GW-501516
    Agonist potency at PPARgamma in CV1 cells by cell based transient transfection assay
    Agonist potency at PPARgamma in CV1 cells by cell based transient transfection assay
    [PMID: 17243659]
    HEK293 EC50
    > 10 μM
    Compound: GW-501516
    Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    Activity at human adipose tissue PPAR gamma expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    [PMID: 17343371]
    HEK293 EC50
    0.002 μM
    Compound: 1, GW-501516
    Agonist activity at Gal4-fused human PPARdelta DNA binding domain expressed in HEK293 cells by luciferase reporter gene assay
    Agonist activity at Gal4-fused human PPARdelta DNA binding domain expressed in HEK293 cells by luciferase reporter gene assay
    [PMID: 21094606]
    HEK293 EC50
    0.0044 μM
    Compound: GW501516
    Agonist activity at GAL4N fused human PPARdelta LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
    Agonist activity at GAL4N fused human PPARdelta LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay
    [PMID: 28539218]
    HEK293 EC50
    0.0059 μM
    Compound: GW501516
    Agonist activity at N-terminal Gal4 fused human PPARdelta LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
    Agonist activity at N-terminal Gal4 fused human PPARdelta LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 27622746]
    HEK293 EC50
    0.0059 μM
    Compound: GW501516
    Agonist activity at GAL4-tagged human PPARdelta ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
    Agonist activity at GAL4-tagged human PPARdelta ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay
    [PMID: 27591006]
    HEK293 EC50
    0.0079 μM
    Compound: GW-501516
    Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    Activity at human placenta PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    [PMID: 17343371]
    HEK293 EC50
    0.054 μM
    Compound: GW-501516
    Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    Agonist activity at mouse PPAR delta expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    [PMID: 17343371]
    HEK293 EC50
    0.085 μM
    Compound: GW-501516
    Agonist activity at human PPARdelta receptor expressed in HEK293 cells by GAL4 transactivation assay
    Agonist activity at human PPARdelta receptor expressed in HEK293 cells by GAL4 transactivation assay
    [PMID: 17524643]
    HEK293 EC50
    0.18 nM
    Compound: GW501516
    Agonist activity at human PPARbeta expressed in HEK293 cells by luciferase reporter gene assay
    Agonist activity at human PPARbeta expressed in HEK293 cells by luciferase reporter gene assay
    [PMID: 25305688]
    HEK293 EC50
    3.9 μM
    Compound: GW-501516
    Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    Activity at human liver PPAR alpha expressed in HEK293 cells by PPAR-GAL4 transactivation assay
    [PMID: 17343371]
    HeLa EC50
    > 10000 nM
    Compound: 27, GW-501516
    Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    Agonist activity at PPARalpha ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    [PMID: 19275963]
    HeLa EC50
    > 10000 nM
    Compound: 27, GW-501516
    Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    Agonist activity at PPARgamma ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    [PMID: 19275963]
    HeLa EC50
    8 nM
    Compound: 27, GW-501516
    Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    Agonist activity at PPARdelta ligand binding domain expressed in human HeLa cells co-transfected with Gal4-DBD assessed as transcriptional activation by Gal4 response element-driven luciferase reporter gene assay
    [PMID: 19275963]
    HepG2 EC50
    0.0012 μM
    Compound: GW-501516
    Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    HepG2 EC50
    0.8 μM
    Compound: GW-501516
    Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    HepG2 EC50
    1.1 μM
    Compound: GW-501516
    Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay
    [PMID: 21215640]
    HepG2 EC50
    4 nM
    Compound: GW-501516
    Agonist activity at human PPARdelta in HepG2 cells by GAL4-luciferase reporter gene assay
    Agonist activity at human PPARdelta in HepG2 cells by GAL4-luciferase reporter gene assay
    [PMID: 17512197]
    In Vitro

    GW 501516 is shown to be the most potent and selective PPARδ agonists known with an EC50 of 1.1 nM against PPARδ and 1000-fold selectivity over the other human subtypes, PPARα and-γ[1].
    GW 501516 exerts anti-inflammatory effects in mouse cultured proximal tubular (mProx) cells. GW 501516 inhibits palmitate- and TNFα-induced increases in MCP-1 mRNA expression in a dose-dependent manner[3].

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

    In Vivo

    GW 501516 causes impaired bone formation, leading to decreased BMD and deterioration of bone properties in OVX rats[2].
    GW 501516 attenuates interstitial inflammation and proximal tubular cell damage in a protein-overload mouse nephropathy model[3].
    GW 501516 treatment enhances running endurance and the proportion of succinate dehydrogenase (SDH)-positive muscle fibres in both trained and untrained mice[4].

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

    Clinical Trial
    Molecular Weight

    453.50

    Formula

    C21H18F3NO3S2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC(COC1=CC=C(C=C1C)SCC2=C(N=C(S2)C3=CC=C(C=C3)C(F)(F)F)C)=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 : ≥ 100 mg/mL (220.51 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2051 mL 11.0254 mL 22.0507 mL
    5 mM 0.4410 mL 2.2051 mL 4.4101 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    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: ≥ 2.5 mg/mL (5.51 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.51 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    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: 99.43%

    References
    Cell Assay
    [3]

    GW 501516 is dissolved in DMSO. Cells are starved by incubation in 0.2% FCS DMEM for 9 h, then pre-incubated with GW 501516, at a final concentration of 2.5 and 5 µM, or 0.05% DMSO as control for 3 hours, followed by stimulation with 150 µM palmitate bound to 8.0% BSA for 12 h[3].

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

    Animal Administration
    [2][3]

    Rats: Female Sprague Dawley rats, 12 weeks of age, are allocated to a sham-operated group and 3 OVX groups; high-dose GW 501516 (OVX-GW5), low-dose GW 501516 (OVX-GW1), and a control group (OVX-CTR), respectively. Animals receive GW 501516 or vehicle (methylcellulose) daily for 4 months by gavage. Bone mineral density (BMD) is assessed by dual x-ray absorptiometry at the femur, spine, and whole body[2].

    Mice: Mice are randomly allocated to different groups and receive therapeutic diet and treatment. The GW 501516-containing rodent diet is made by evenly adding GW 501516 to the control diet to a final concentration of 0.04% w/w. In the control diet, 10% of the total calories are from fat (5.5% from soybean oil and 4.5% from lard)[3].

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

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2051 mL 11.0254 mL 22.0507 mL 55.1268 mL
    5 mM 0.4410 mL 2.2051 mL 4.4101 mL 11.0254 mL
    10 mM 0.2205 mL 1.1025 mL 2.2051 mL 5.5127 mL
    15 mM 0.1470 mL 0.7350 mL 1.4700 mL 3.6751 mL
    20 mM 0.1103 mL 0.5513 mL 1.1025 mL 2.7563 mL
    25 mM 0.0882 mL 0.4410 mL 0.8820 mL 2.2051 mL
    30 mM 0.0735 mL 0.3675 mL 0.7350 mL 1.8376 mL
    40 mM 0.0551 mL 0.2756 mL 0.5513 mL 1.3782 mL
    50 mM 0.0441 mL 0.2205 mL 0.4410 mL 1.1025 mL
    60 mM 0.0368 mL 0.1838 mL 0.3675 mL 0.9188 mL
    80 mM 0.0276 mL 0.1378 mL 0.2756 mL 0.6891 mL
    100 mM 0.0221 mL 0.1103 mL 0.2205 mL 0.5513 mL
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    Product Name:
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    Cat. No.:
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