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Chemical Structure| 188591-46-0 Chemical Structure| 188591-46-0

Structure of GSK3787
CAS No.: 188591-46-0

Chemical Structure| 188591-46-0

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

Synonyms: GSK3787

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Product Details of GSK3787

CAS No. :188591-46-0
Formula : C15H12ClF3N2O3S
M.W : 392.78
SMILES Code : O=C(NCCS(=O)(C1=NC=C(C(F)(F)F)C=C1)=O)C2=CC=C(Cl)C=C2
Synonyms :
GSK3787
MDL No. :MFCD00099612
InChI Key :JFUIMTGOQCQTPF-UHFFFAOYSA-N
Pubchem ID :2800647

Safety of GSK3787

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H317-H319
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • PPARβ/δ

    PPARδ, pIC50:6.6

  • PPARδ

    PPARδ, pIC50:6.6

In Vitro:

Cell Line
Concentration Treated Time Description References
rat pulmonary artery cells 1 μM 24 hours GSK3787 alone had no significant effect on LPS-induced NO and IL-6 release in rat pulmonary artery, but co-incubation with GW0742 significantly reduced NO and IL-6 production. PMC8003823
porcine corpus luteum cells 25 μM 6 hours To investigate the effect of GSK3787 on LPS-induced inflammation in porcine corpus luteum cells, the results showed that GSK3787 affected the expression of 88 differentially expressed genes. PMC10003567
HCT116 cells 1 μM 24 hours GSK3787 decreased c-Myc mRNA expression PMC6397663
SW620 cells 1 μM 24 hours GSK3787 reduced active β-catenin levels PMC6397663
CT26 cells 1.0 μM 48 hours GSK3787 blocked PPARD’s promotion of cell invasion PMC6397663
AGS human gastric cancer cells 2 µg/mL 48 hours To investigate the effect of PPARδ overexpression on CCL20 mRNA expression, results showed that PPARδ significantly upregulated CCL20 expression in AGS cells. PMC10640489
N87 human gastric cancer cells 2 µg/mL 48 hours To investigate the effect of PPARδ overexpression on CCL20 mRNA expression, results showed that PPARδ significantly upregulated CCL20 expression in N87 cells. PMC10640489
Mouse gastric cancer cells 2 µg/mL 48 hours To investigate the effect of PPARδ overexpression on CCL20 mRNA expression, results showed that PPARδ significantly upregulated CCL20 expression in mouse gastric cancer cells. PMC10640489

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
rats Neonatal hypoxic-ischemic brain injury model Intranasal administration 300 μg/kg 1 hour before HI and 24 hours post HI GSK3787 significantly reversed the protective effects of GW0742, leading to increased infarct area and impaired neurological function PMC6223650
Sprague-Dawley rats Hypoxic-ischemic brain injury model Intranasal administration 300 μg/kg Administered 1 hour before HI and 24 hours post-HI GSK3787 significantly increased NLRP3 expression, reversing the anti-inflammatory effects of GW0742 and leading to a significant increase in TNF-α expression. PMC7686982
Mice ApcΔ580 mice Oral 200 mg/kg for 12 consecutive weeks GSK3787 significantly reduced colonic tumor numbers and sizes PMC6397663
PpardTG mice PpardTG mouse model Oral 200 mg/kg 44 weeks To investigate the inhibitory effect of GSK3787 on gastric cancer carcinogenesis in PpardTG mice, results showed that GSK3787 significantly suppressed the development and progression of gastric cancer. PMC10640489

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.73mL

2.55mL

1.27mL

25.46mL

5.09mL

2.55mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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