ABP/PPAR modulator 1
ABP/PPAR modulator 1 is an orally active FABP and PPAR multiple modulator (IC50s of 0.65 μM and 1.08 μM for FABP1 and FABP4, EC50 s of 9.19 μM, 2.20 μM and 1.58 μM for PPARα, PPARγ and PPARδ). ABP/PPAR modulator 1 has potent anti-metabolic dysfunction-associated steatohepatitis (MASH) activity. ABP/PPAR modulator 1 dose-dependently ameliorates multiple pathological characteristics of fatty liver in WD + Carbon tetrachloride-induced MASH mice model.
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- CAS No.: 3104894-76-7
- Formule: C33H39NO7
- Masse moléculaire:561.67
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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PPARα 9.19 μM (EC50) |
PPARγ 2.20 μM (EC50) |
PPARδ 1.58 μM (EC50) |
FABP1 0.65 μM (IC50) |
FABP4 1.08 μM (IC50) |
ABP/PPAR modulator 1 (Compound 27) has superior binding capacity on PPARs (Kds of 5.23 μM, 0.98 μM and 0.76 μM for PPARα, PPARγ and PPARδ)[1].
ABP/PPAR modulator 1 (10 mM-0.1 μM) shows higher affinity for FABP1 than its endogenous ligand, linoleic acid (LA) (Kd: 5.885 μM vs. LA: 14.281 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ABP/PPAR modulator 1 (20 mg/kg, p.o., once a day for 4 weeks) significantly reduces TC and hepatic TG levels in MASH mice model[1].
ABP/PPAR modulator 1 (10 mg/kg, p.o., once a day for 4 weeks) significantly decreases the levels of liver LDH, serum AST, ALT, TBA, and TBIL, and does not affect the ALP level in MASH mice model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:male C57BL/6 mice (6 weeks old) were given a high-sugar diet (18.9 g/L glucose and 23.1 g/L fructose) and a high-fat feed (41 % sucrose, 21.1 % fat, and 1.25 % cholesterol) with 2 % CCl4 olive oil (i.p., once a week for 12 weeks) to induce MASH
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Dosage:5, 10, 20 mg/kg
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Administration:p.o., once a day for 4 weeks, and then collects liver tissues.
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Result:Dose-dependently reduced the liver weight, the liver weight to body weight ratio and NAS scores of MASH mice, with its anti-MASH efficacy significantly improving as the dosage increased.
Dose-dependently decreased MPO expression levels and downregulated MCP-1, TNF-α, IL-1β, and IL-6 mRNA expression in MASH mice model.
Significantly reduced the levels of liver of TC, hepatic TG levels liver LDH, serum AST, ALT, TBA, and TBIL, and did not affect the ALP level in MASH mice model.
Increased the levels of SOD, GSH-Px, and GST, and decreased MDA content, protecting the liver from oxidative stress in MASH mice model.
Significantly reduced the expression ofα-SMA, TGF-β and HYP levels, inhibiting the activation of hepatic stellate cells and the liver fibrosis in MASH mice model.
Chemical Information
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CAS No. 3104894-76-7
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Masse moléculaire 561.67
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Formule C33H39NO7
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SMILES
COC1=CC=C(/C=C/C2=CC(OCC3=CC=C(OC(C)(C)C(N[C@@H](C(O)=O)CC(C)C)=O)C=C3)=CC(OC)=C2)C=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ABP/PPAR modulator 1 Related Classifications
HY-172883 Related Classifications
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