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Cat. No.: HY-10839

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L-165461

L-165461 is a PPARδ and PPARγ agonist with K_i values of 3 nM and 15 nM, respectively. L-165461 can be used for research on diabetes.

For research use only. We do not sell to patients.

CAS No.: 194608-76-9
Formula: C₂₃H₂₆ClNO₄S
Molecular Weight:447.97

Storage:

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

L-165461 Chemical Structure

CAS No.: 194608-76-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

L-165461 is a PPARδ and PPARγ agonist with K_i values of 3 nM and 15 nM, respectively. L-165461 can be used for research on diabetes^[1]^[2]^[3].

IC₅₀ & Target

^[1]

PPARγ

15 nM (Ki)

PPARδ

3 nM (Ki)

All PPAR Isoforms :

In Vitro

Lipid MetabolismInnate ImmunityCytokines and ChemokinesOthers

Lipid Metabolism

L-165461 (4 days) promotes preadipocyte differentiation in 3T3-L1 cells, as measured by aP2 mRNA expression, consistent with its PPARγ binding affinity^[1].

Innate Immunity

Cytokines and Chemokines

L-165461 (50 μM; 1 h) does not inhibit LPS-induced TNF-α or IL-6 production in freshly isolated or 5-day cultured human monocytes^[2].
L-165461 (50 μM; 1 h) does not inhibit PMA-induced TNF-α or IL-6 production in freshly isolated or 5-day cultured human monocytes^[2].
L-165461 (50 μM; 1 h) does not inhibit LPS-induced TNF-α production in murine RAW 264.7 macrophage-like cells^[2].

Others

L-165461 (~16 h) is a potent dual ligand for both PPARγ (K_i = 15 nM) and PPARδ (K_i = 3 nM)^[1].
L-165461 (48 h) acts as an agonist for both hPPARγ and hPPARδ, producing robust transactivation of the UAS reporter gene in COS-1 cells expressing either receptor^[1].
L-165461 binds to and activates the human PPARδ ligand binding domain with an EC₅₀ of 0.012 µM^[3].

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

ELISA Assay^[2]

Cell Line:

Human peripheral blood monocytes
Concentration:

50 μM
Incubation Time:

1 h (pre-treatment); 4 h (LPS stimulation)
Result:

Failed to inhibit LPS-induced TNF-α or IL-6 synthesis and secretion at concentrations up to 50 μM.

ELISA Assay^[2]

Cell Line:

Human peripheral blood monocytes
Concentration:

50 μM
Incubation Time:

1 h (pre-treatment); 18-24 h (PMA stimulation)
Result:

Failed to inhibit PMA-induced TNF-α or IL-6 synthesis and secretion at concentrations up to 50 μM.

Related Protocols :

Research Protocol for Metabolic Diseases

Chemical Information

CAS No. 194608-76-9
Molecular Weight 447.97
Formula C₂₃H₂₆ClNO₄S
SMILES

O=C(CC1=CC=C(C(Cl)=C1)SCCCOC2=C(CCC)C(ON=C3CC)=C3C=C2)O
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]. Berger J, et al. Novel peroxisome proliferator-activated receptor (PPAR) gamma and PPARdelta ligands produce distinct biological effects. The Journal of biological chemistry. 1999 Mar 05;274(10):6718-25. [Content Brief]

[2]. Thieringer R, et al. Activation of peroxisome proliferator-activated receptor γ does not inhibit IL-6 or TNF-α responses of macrophages to lipopolysaccharide in vitro or in vivo[J]. The Journal of Immunology, 2000, 164(2): 1046-1054.

[3]. Epple R, et al. Novel bisaryl substituted thiazoles and oxazoles as highly potent and selective peroxisome proliferator-activated receptor delta agonists. Journal of medicinal chemistry. 2010 Jan 14;53(1):77-105.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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L-165461

All PPAR Isoforms

Biological Activity

Description

IC50 & Target

In Vitro

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

L-165461 Related Classifications

HY-10839 Related Classifications

Bioz

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