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L-165041

SKU: orb1300017

Description

L-165041 is a potent and selective agonist for PPARβ/δ, exhibiting high binding affinity (Ki = 9 nM) and functional activity (EC50 ~500 nM). This tool compound is widely used in metabolic, inflammatory, and muscle physiology research, supporting both in vitro mechanistic studies and in vivo preclinical models.

Research Area

Metabolism Research, Molecular Biology

Images & Validation

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L-165041

Key Properties

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CAS Number79558-09-1
MW402.44
Purity97.97%
FormulaC22H26O7
SMILESCCCc1c(O)c(ccc1OCCCOc1ccc(OCC(O)=O)cc1)C(C)=O
TargetPPAR
SolubilityDMSO:50 mg/mL (124.24 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.97 mM)

Bioactivity

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Target IC50
PPARβ:9 nM(Ki)|PPARδ:500 nM(EC50)|PPARγ:730 nM (Ki)
In Vivo
L-165041 lowered hepatic expression of PPARgamma, apolipoprotein B, interleukin 1 beta (IL-1beta), and interleukin-6. In contrast, L-165041 increased hepatic expressions of PPARdelta, lipoprotein lipase (LPL), and ATP-binding cassette transporter G1 (ABCG1).L-165041 might be effective in preventing Western diet-induced hepatic steatosis by regulating genes involved in lipid metabolism and the inflammatory response.
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In Vitro
L-165041 inhibited VEGF-induced cell proliferation and migration in human umbilical vein ECs (HUVECs). L-165041 also inhibited angiogenesis in the Matrigel plug assay and aortic ring assay. Flow cytometric analysis indicated that L-165041 reduced the number of ECs in the S phase and the expression levels of cell cycle regulatory proteins such as cyclin A, cyclin E, CDK2, and CDK4; phosphorylation of the retinoblastoma protein was suppressed by pretreatment with L-165041. The PPARδ ligand L-165041 inhibits VEGF-stimulated angiogenesis by suppressing the cell cycle progression independently of PPARδ.
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Cell Research
Cell cycle distribution was determined by flow cytometry. Synchronized HUVECs were pretreated with L-165041 (1 or 5μM) 6 h prior to the addition of VEGF (10 ng/ml). The cells were harvested 16 h after VEGF addition and washed with PBS. The cells were then incubated with buffer containing 0.1% Triton X-100 and 0.1% trisodium citrate for 30 min. Cells were rinsed with PBS and then stained with 50 μg/ml propidium iodide for 20 min at room temperature. In total, 1*10^4 cells were analyzed with the FACScan system . At least three independent experiments were performed.
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Animal Research
The effect of PPARdelta ligand L-165041 on Western diet-induced fatty liver using low-density lipoprotein receptor-deficient (LDLR(-/-)) mice. LDLR(-/-) mice received either L-165041 (5mg/kg/day) or vehicle (0.1N NaOH) with Western diet for 16 weeks. L-165041 drastically reduced lipid accumulation in the liver, decreasing total hepatic cholesterol and triglyceride content compared to the vehicle group.
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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inhibit, L 165041, Inhibitor, L165041, L-165041, PPAR, Peroxisome proliferator-activated receptors

Similar Products

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  • L-165041

    L-165041 [orb1220484]

    >98% (HPLC)

    79558-09-1

    402.4

    C22H26O7

    2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg, 1 g, 500 mg, 200 mg
Quality Guarantee

Quality Guarantee

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Compound Identifiers

PubChem CID
6603901 ↗

Key Properties

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No computed properties available.

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L-165041 (orb1300017)

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% Tween 80 +
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Available Sizes

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5 mg
¥ 1,040.00
1 ml x 10 mM (in DMSO)
¥ 1,170.00
10 mg
¥ 1,430.00
25 mg
¥ 2,210.00
50 mg
¥ 3,510.00
100 mg
¥ 5,200.00
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