1. Cell Cycle/DNA Damage
  2. PPAR
  3. GSK3787

GSK3787 

Cat. No.: HY-15577 Purity: 96.67%
Handling Instructions

GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.

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

GSK3787 Chemical Structure

GSK3787 Chemical Structure

CAS No. : 188591-46-0

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 117 In-stock
Estimated Time of Arrival: December 31
10 mg USD 106 In-stock
Estimated Time of Arrival: December 31
50 mg USD 451 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 7 publication(s) in Google Scholar

Top Publications Citing Use of Products

    GSK3787 purchased from MCE. Usage Cited in: Nutrition. 2019 Apr;60:217-226.

    Leu and HMB stimulate the protein expression of PPARβ/δ and CDK4, and GSK3787 and LY2835219 block the protein expression of PPARβ/δ and CDK4.

    GSK3787 purchased from MCE. Usage Cited in: Nutrition. 2019 Apr;60:217-226.

    The mRNA expression levels of AMPKα, Sirt1, PGC-1α change significantly with the treatment of GSK3787 or LY2835219 are showed.

    GSK3787 purchased from MCE. Usage Cited in: Nutrition. 2019 Apr;60:217-226.

    The mRNA expression levels of Nrf-1, TFAM, MEF-2A, MEF-2CD, and MEF-2C change significantly with the treatment of GSK3787 or LY2835219 are showed.

    GSK3787 purchased from MCE. Usage Cited in: Nutrition. 2019 Apr;60:217-226.

    GSK3787 significantly reverse the beneficial effects of Leu and HMB on mitochondrial mass.

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    Description

    GSK3787 is a selective and irreversible peroxisome proliferator-activated receptor δ (PPARδ) antagonist with pIC50 of 6.6.

    IC50 & Target[1]

    PPARδ

    6.6 nM (pIC50)

    In Vitro

    GSK3787 is identified as a potent and selective hPPARδ ligand (pIC50=6.6) with no measurable affinity for hPPARα or hPPARγ (pIC50 < 5) in our standard in vitro ligand displacement assay. GSK3787 is inactive against hPPARα and hPPARγ in similar functional antagonist assays. GSK3787 fails to activate the receptor in a standard hPPARδ-GAL4 chimera cell-based reporter assay. GSK3787 is a selective PPARδ antagonist with equipotent species activity against the human and mouse receptor[1].

    In Vivo

    GSK3787 has pharmacokinetic properties suitable for use as an in vivo PPARδ antagonist tool compound in mice. GSK3787 is administered intravenously (0.5 mg/kg) and orally (10 mg/kg) to male C57BL/6 mice. Mean clearance (CL) and volume of distribution at steady state (Vss) following iv administration are 39±11 (mL/min)/kg and 1.7±0.4 L/kg, respectively. Following oral administration, good exposure (Cmax=881±166 ng/mL, AUCinf=3343±332 h•ng/mL), half-life (2.7±1.1 h), and bioavailability (F=77±17%) are observed[1]. Oral administration of GSK3787 (10 mg/kg) leads to a serum Cmax of 2.2±0.4 μM in C57BL/6 male mice. Oral administration of GW0742 causes an increase in expression of Angptl4 and Adrp mRNA (known PPARβ/δ target genes) in wild-type mouse colon epithelium, and this effect is not found in Pparβ/δ-null mouse colon epithelium. Coadministration of GSK3787 with GW0742 effectively prevents the ligand-induced expression of both Angptl4 and Adrp mRNA in wild-type mouse colon epithelium, and this effect is not found in Pparβ/δ-null mouse colon epithelium. Oral administration of GSK3787 causes a modest increase in promoter occupancy of PPARβ/δ in the PPRE region of both the Angptl4 and Adrp genes, but coadministration of GSK3787 with GW0742 results in markedly less accumulation of PPARβ/δ in the PPRE region of both the Angptl4 and Adrp genes in wild-type mouse colon epithelium[2].

    Molecular Weight

    392.78

    Formula

    C₁₅H₁₂ClF₃N₂O₃S

    CAS No.

    188591-46-0

    SMILES

    O=C(NCCS(=O)(C1=NC=C(C(F)(F)F)C=C1)=O)C2=CC=C(Cl)C=C2

    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 : ≥ 50 mg/mL (127.30 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5460 mL 12.7298 mL 25.4595 mL
    5 mM 0.5092 mL 2.5460 mL 5.0919 mL
    10 mM 0.2546 mL 1.2730 mL 2.5460 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: 2.5 mg/mL (6.36 mM); Suspended solution; Need ultrasonic

    • 2.

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

      Solubility: ≥ 2.5 mg/mL (6.36 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Animal Administration
    [2]

    Mice[2]
    For RNA and DNA analysis, male wild-type and Pparβ/δ-null mice are administered vehicle (corn oil), GW0742 (10 mg/kg), GSK3787 (10 mg/kg), or GW0742 and GSK3787 by oral gavage 3 h before euthanasia. After euthanasia, colons are carefully dissected. To isolate colon epithelium, colons are flushed with phosphate-buffered saline, and epithelial cells are scraped from mucosa using a razor blade. The isolated tissues are used for RNA isolation. For glucose-tolerance tests, male wild-type and Pparβ/δ-null mice are administered vehicle (corn oil), GW0742 (10 mg/kg), GSK3787 (10 mg/kg), or Rosiglitazone (20 mg/kg) by oral gavage once a day for 2 weeks.

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

    References
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    Product name:
    GSK3787
    Cat. No.:
    HY-15577
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