GSK3787

Catalog No.S8025

GSK3787 Chemical Structure

Molecular Weight(MW): 392.78

GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.

Size Price Stock Quantity  
In DMSO USD 140 In stock
USD 110 In stock
USD 470 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

1 Customer Review

  • (b) Western blotting used to analyze the expression of caspase-12. The caspase-12 levels were quantified and normalized to the GAPDH levels (n=6; F=23.785>F0.01(3, 20); ∗∗P < 0.01 vs. Con group; ##P < 0.01 vs. Cort group; ††P < 0.01 vs. GW group); (c) Western blotting used to analyze the ratio of cleaved caspase-3 to caspase-3 of the different groups (n=4; F=10.419>F0.01(3, 12); ∗∗P < 0.01 vs. Con group; #P < 0.05 vs. Cort group; †P < 0.05 vs. GW group). Groups were compared using 1-way ANOVA with post hoc Tukey's multiple comparisons test. The data are presented as the mean ± SEM. Con, Control; Cort, Corticosterone; GW, GW0742; GSK, GSK3787

    Neuropharmacology, 2016, 113(Pt A):396-406. . GSK3787 purchased from Selleck.

Purity & Quality Control

Choose Selective PPAR Inhibitors

Biological Activity

Description GSK3787 is as a selective and irreversible antagonist of PPARδ with pIC50 of 6.6, with no measurable affinity for hPPARα or hPPARγ.
Targets
PPARδ [1]
6.6(pIC50)
In vitro

GSK3787 irreversibly antagonizes human and mouse PPARδ that covalently modifies Cys249 within the ligand binding pocket. GSK 3787 completely antagonizes the activity of agonist GW501516 with a pIC50 of 6.9 and 94% maximal inhibition. GSK3787 (1 μM) effectively antagonizes the agonist GW0742 stimulated transcription of CPT1a and PDK4 in human skeletal muscle cells, and effectively antagonize the basal gene expression of CPT1a. GSK 3787 shows no effective antiproliferative activity against colorectal cancer cells. [1] GSK3787 (1 μM) completely antagonizes 50 nM GW0742-induced PPARβ/δ-dependent Angptl4 gene expression in wild-type fibroblasts and in keratinocytes. GSK3787 (1 μM) largely antagonizes 50 nM GW0742-induced Angptl4 and Adrp mRNAs expression in skin cancer cell A341. GSK3787 (1 μM) largely antagonizes GW0742-induced Angptl4 mRNAs expression in cancer cell lines MCF7 (breast), Huh7 (liver), and HepG2 (liver) cells but not in H1838 or A549 cells (lung). GSK3787 (1 μM) largely antagonizes GW0742-induced increase of Adrp mRNA in Huh7 and HepG2 cells but not in H1838 cells. GSK3787 does not antagonize basal expression of either of these two PPARβ/δtarget genes in these cells. Neither GW0742 nor GSK3787 has any effect on cell proliferation of these cells at concentrations ranging from 0.1 to 10 μM. GSK3787 is able to modulate the association of both PPARβ/δ and PPARγ coregulator peptides in response to ligand activation. Efficacy of GSK3787 to modulate PPARγ activity is markedly lower than the efficacy of GSK3787 to act as a PPARβ/δ antagonist. [2]

In vivo GSK3787 antagonizes ligand-induced PPARβ/δ-dependent gene expression in vivo. Oral administration of GSK3787 has no effect on the expression of Angptl4 and Adrp mRNA in mouse colon epithelium. Coadministration of GSK3787 (10 mg/kg) effectively prevents the GW0742-induced expression of both Angptl4 and Adrp mRNA in wild-type mouse colon epithelium, which is correlated with reduced promoter occupancy of PPARβ/δ on the Angptl4 and Adrp genes. Administration of GSK3787 had no effect on glucose tolerance. [2]

Protocol

Solubility (25°C)

In vitro DMSO 79 mg/mL (201.13 mM)
Water <1 mg/mL
Ethanol <1 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 392.78
Formula

C15H12ClF3N2O3S

CAS No. 188591-46-0
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

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

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

PPAR Signaling Pathway Map

Related PPAR Products

Tags: buy GSK3787 | GSK3787 supplier | purchase GSK3787 | GSK3787 cost | GSK3787 manufacturer | order GSK3787 | GSK3787 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID