ABP/PPAR modulator 1

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ABP/PPAR modulator 1 is a first-in-class FABP and PPAR multiple modulator (IC₅₀s of 0.65  μM and 1.08  μM for FABP1 and FABP4, EC₅₀s 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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ABP/PPAR modulator 1 Chemical Structure

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PPARα PPARβ/δ PPARγ PPAR PPARδ

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

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)

In Vitro

ABP/PPAR modulator 1 (Compound 27) has superior binding capacity on PPARs (K_ds 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) (K_d: 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.

In Vivo

ABP/PPAR modulator 1 (Compound 27) (5-20 mg/kg, p.o., once a day for 4 weeks) dose-dependently reduces the liver weight, the liver weight to body weight ratio and NAS scores while inhibiting inflammation, attenuating fibrosis, and alleviating oxidative stress in Western diet combined with low-dose Carbon tetrachloride (HY-Y0298) (CCl4) (WD + Carbon tetrachloride) induced MASH mice, with anti-MASH efficacy strengthening at higher doses^[1].
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.

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
Dosage:	5, 10, 20 mg/kg
Administration:	p.o., once a day for 4 weeks, and then collects liver tissues.
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.

Molecular Weight

561.67

Formula

C₃₃H₃₉NO₇

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Chen Y, et al. Discovery of the first-in-class FABP/PPAR multiple modulator for the treatment of metabolic dysfunction-associated steatohepatitis. Eur J Med Chem. 2025 Jul 5; 291:117635. [Content Brief]