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  3. GSK3787

GSK3787 

Cat. No.: HY-15577 Purity: 99.04%
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  
Solution
10 mM * 1 mL in DMSO USD 117 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 117 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 106 In-stock
Estimated Time of Arrival: December 31
50 mg USD 451 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Customer Review

Based on 11 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].

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

    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].

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

    Molecular Weight

    392.78

    Formula

    C15H12ClF3N2O3S

    CAS No.
    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)

    *"≥" 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 available 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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