2. Cell Cycle/DNA Damage Vitamin D Related/Nuclear Receptor Metabolic Enzyme/Protease Membrane Transporter/Ion Channel
  3. PPAR ATP-binding cassette (ABC) transporters
  4. PPAR agonist 8

PPAR agonist 8 is an orally active pan-PPAR agonist, with KD values of 0.576 μM, 2.06 μM and 1.45 μM for PPARα, PPARγ and PPARδ, respectively. PPAR agonist 8 upregulates the expression of ATP-binding cassette transporter A1 (ABCA1) and promotes cholesterol efflux. PPAR agonist 8 reduces plasma cholesterol levels, decreases cholesterol accumulation in the liver and cholesterol deposition in pancreatic islets, regulates glucose and lipid metabolism, and causes no side effects of weight gain and obesity. PPAR agonist 8 can be used in the research of type 2 diabetes, hepatic steatosis and pancreatic islet dysfunction.

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PPAR agonist 8

PPAR agonist 8 Chemical Structure

CAS No. : 1031072-40-8

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PPAR agonist 8 Related Antibodies

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Description

PPAR agonist 8 is an orally active pan-PPAR agonist, with KD values of 0.576 μM, 2.06 μM and 1.45 μM for PPARα, PPARγ and PPARδ, respectively. PPAR agonist 8 upregulates the expression of ATP-binding cassette transporter A1 (ABCA1) and promotes cholesterol efflux. PPAR agonist 8 reduces plasma cholesterol levels, decreases cholesterol accumulation in the liver and cholesterol deposition in pancreatic islets, regulates glucose and lipid metabolism, and causes no side effects of weight gain and obesity. PPAR agonist 8 can be used in the research of type 2 diabetes, hepatic steatosis and pancreatic islet dysfunction[1].

IC50 & Target[1]

PPARα

0.576 μM (Kd)

PPARγ

2.06 μM (Kd)

PPARδ

1.45 μM (Kd)

In Vitro

PPAR agonist 8 (Compound 15a) potently and evenly activates hPPARα, hPPARγ and hPPARδ in HepG2 cells, with EC50 values of 6.94 μM, 13.87 μM and 3.83 μM, respectively[1].
PPAR agonist 8 (24 h) potently upregulates the activity of the ABCA1 promoter in HepG2 cells, with an EC50 of 4.27 μM and a maximum activation rate of 431% relative to DMSO[1].
PPAR agonist 8 (10 μM; 40 min) enhances glucose-stimulated insulin secretion in INS-1 cells in an ABCA1-dependent manner[1].
PPAR agonist 8 (1-10 μM; 7 days) does not significantly promote adipogenic differentiation or lipid accumulation in 3T3-L1 preadipocytes, thus avoiding the adipogenic side effects of selective PPARγ agonists[1].
PPAR agonist 8 (30 μM) exhibits only 20.72% inhibition of the hERG K+ channel, indicating a low risk of QT interval prolongation[1].

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

PPAR agonist 8 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ CL F
Rat[1] 5 mg/kg i.v. 0.34 h 0.083 h 4687.03 ng/mL 1347.46 ng·h/mL 1348.83 ng·h/mL 63.14 mL/min/kg /
Rat[1] 50 mg/kg p.o. 1.69 h 0.58 h 791.75 ng/mL 1226.04 ng·h/mL 1252.48 ng·h/mL / 9.10 %
In Vivo

PPAR agonist 8 (Compound 15a) (50 mg/kg; p.o.; daily; 24 days) significantly improves glucose homeostasis, lipid metabolism, hepatic steatosis, and islet function in high fat and high glucose die (HFHGD)-induced T2DM KKAy mice while avoiding weight gain and adipogenic side effects associated with selective PPARγ agonists[1].

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

Animal Model: KKAy mice (male, 6-week-old, high fat and high glucose diet-induced T2DM model)[1]
Dosage: 50 mg/kg
Administration: p.o.; daily; 24 days
Result: Restored body weight to near-normal control levels, avoiding weight gain associated with RGZ treatment.
Markedly decreased plasma total cholesterol (TC) and triglyceride (TG) levels.
Surpassed RGZ in reducing fasting blood glucose and homeostatic model assessment of insulin resistance (HOMA-IR) levels.
Significantly improved oral glucose tolerance tests (OGTT) and insulin tolerance tests (ITT) area under the curve (AUC) values.
Reduced liver weight, liver weight-to-body weight ratio, hepatic TC and TG accumulation, and cholesterol deposition in liver tissue; promoted fecal cholesterol excretion; decreased plasma alanine transaminase (ALT) levels.
Ameliorated hepatic steatosis and lipid accumulation as shown by H&E and Oil Red O staining.
Upregulated hepatic mRNA expression of glucose metabolism-related genes (glucokinase (Gck), glucose transporter 2 (Glut2), insulin receptor substrate 1 (Irs1)) and cholesterol efflux genes (ATP binding cassette subfamily A member 1 (Abca1), ATP binding cassette subfamily G member 5 (Abcg5), ATP binding cassette subfamily G member 8 (Abcg8)); downregulated hepatic mRNA expression of gluconeogenic genes (glucose-6-phosphatase (G6pc), fructose-Bisphosphatase 2 (Fbp2)), cholesterol synthesis gene (3-hydroxy-3-methylglutaryl-CoA synthase 1 (Hmgcs1)), adipogenesis-related factors (cluster of differentiation 36 (Cd36), stearoyl-CoA desaturase (Scd1), ELOVL fatty acid elongase 6 (Elovl6), Pparγ1), and inflammatory cytokines (Il1α, Il1β); increased hepatic mRNA expression of Pparα and Pparδ.
Ameliorated islet hypertrophy, disorganized islet cell arrangement, and islet cholesterol accumulation; increased islet ABCA1 expression and insulin secretion.
Reduced epididymal and subcutaneous white adipose tissue (eWAT, sWAT) mass, avoided adipogenic side effects of RGZ, and ameliorated adipocyte hypertrophy and adipose tissue macrophage infiltration.
Molecular Weight

258.23

Formula

C13H10N2O4
CAS No.
SMILES

O=C(NC1=NC=CC=C1O)C2=CC(OCO3)=C3C=C2
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Purity & Documentation
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PPAR agonist 8 Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PPAR agonist 81031072-40-8PPAR agonist8PPAR agonist-8PPARATP-binding cassette (ABC) transportersPeroxisome proliferator-activated receptorsATP-binding cassette transportershepatic steatosisHepG2 cellsligand binding domainINS-1 cells3T3-L1 preadipocytestype 2 diabetes mellitusATP binding cassette transporter A1PPARαPPARγPPARδInhibitorinhibitorinhibit

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