KRP-297
KRP-297 is a PPARα and PPARγ agonist potentially for the research of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver.
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- CAS. Nr.: 213252-19-8
- Formel: C20H17F3N2O4S
- Molecular Weight:438.42
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
0.8 μM
Compound: 4 (KRP-297)
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Concentration of compound that affords half-maximum transactivation of human Peroxisome proliferator activated receptor gamma in CHO-K1 cells was determined in vitro
Concentration of compound that affords half-maximum transactivation of human Peroxisome proliferator activated receptor gamma in CHO-K1 cells was determined in vitro
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[PMID: 11738577] |
| CHO-K1 | EC50 |
1 μM
Compound: 4 (KRP-297)
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Transactivation of human Peroxisome proliferator activated receptor alpha expressed in CHO-K1 cells
Transactivation of human Peroxisome proliferator activated receptor alpha expressed in CHO-K1 cells
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[PMID: 11738577] |
| CV-1 | EC50 |
>10 μM
Compound: KRP-297
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Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
Agonist activity at human PPARdelta-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
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[PMID: 21515063] |
| CV-1 | EC50 |
0.4 μM
Compound: KRP-297
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Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
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[PMID: 21515063] |
| CV-1 | EC50 |
0.9 μM
Compound: KRP-297
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Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay
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[PMID: 21515063] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 213252-19-8
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Molecular Weight 438.42
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Formel C20H17F3N2O4S
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SMILES
O=C(C1=CC(CC2SC(NC2=O)=O)=CC=C1OC)NCC3=CC=C(C=C3)C(F)(F)F
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Synonyms
MK-0767
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[1]. Murakami K, Tobe K, Ide T, et al. A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-alpha (PPAR-alpha) and PPAR-gamma: effect of PPAR-alpha activation on abnormal lipid metabolism in liver of Zucker fatty rats. Diabetes. 1998;47(12):1841-1847. [Content Brief]
[2]. Kochansky CJ, Rippley RK, Yan KX, et al. Absorption, metabolism, and excretion of [14C]MK-0767 (2-methoxy-5-(2,4-dioxo-5-thiazolidinyl)-N-[[4-(trifluoromethyl)phenyl] methyl]benzamide) in humans. Drug Metab Dispos. 2006;34(9):1457-1461. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
KRP-297 Related Classifications
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