YS121
Based on 1 Customer Validation
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM). YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells. YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively). YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research.
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- Pureza: 99.74%
- No. CAS: 916482-17-2
- Fòrmula: C20H26ClN3O2S
- Peso molecular:407.96
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Almacenamiento:
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Chemical Information
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Solvente y solubilidad
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Actividad biológica
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PPAR-α 1 μM (EC50) |
PPAR-γ 3.6 μM (EC50) |
5-Lipoxygenase 6.5 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
12 μM
Compound: 2d
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Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation by cell-intact assay
Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation by cell-intact assay
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[PMID: 19053751] |
| A549 | IC50 |
3.9 μM
Compound: 2d
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Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay
Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay
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[PMID: 19053751] |
| COS-7 | EC50 |
1 μM
Compound: 3
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Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
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[PMID: 25022880] |
| COS-7 | EC50 |
3.6 μM
Compound: 2
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Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay
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[PMID: 20307981] |
| COS-7 | EC50 |
3.6 μM
Compound: 3
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Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay
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[PMID: 25022880] |
| COS-7 | IC50 |
1 μM
Compound: 2
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Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
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[PMID: 25037914] |
| COS-7 | IC50 |
3.6 μM
Compound: 2
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Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
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[PMID: 25037914] |
| PMNL | IC50 |
4.1 μM
Compound: 2d
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Inhibition of 5-LO in PMNL cells
Inhibition of 5-LO in PMNL cells
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[PMID: 19053751] |
YS121 (0.3-30 μM) acts as a potent and selective inhibitor of mPGES-1 in interleukin-1β-stimulated human A549 cell microsomes, concentration-dependently and non-competitively blocking the conversion of PGH2 to PGE2, with no marked inhibition of other PGES enzymes[1].
YS121 (0.1-30 μM) concentration-dependently inhibits PGE2 formation with an IC50 value of 3 μM, and moderately suppresses PGE2 synthesis in the absence of CV4151[1].
YS121 (0.1-30 μM) inhibits PGE2 formation without affecting the synthesis of COX-2-derived 6-keto PGF1α and TxB2 or COX-1-derived 12-HHT in human whole blood[1].
YS121 (10 μM, 0-48 h) selectively modulates protein expression over a 48-hour period, specifically reducing COX-2 levels after 24 hours while leaving mPGES-1 expression unchanged[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:interleukin-1β-stimulated human A549 cells
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Concentration:10 μM
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Incubation Time:0, 12, 24, and 48 h
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Result:Decreased the levels of COX-2 after 24 to 48 h in interleukin-1β-stimulated human A549 cells.
Had no significant impact on mPGES-1 expression levels over 48 hours.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male adult Wistar Han rats (200-220 g) injected intraperitoneally with carrageenan[1]
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Dosage:1.5 mg/kg
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Administration:i.p., 30 min pre-modeling, once
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Result:Significantly inhibited the exudate formation by 62 % and cell infiltration by 40 %.
Reduced the levels of PGE2, LTB4 and 6-keto PGF1α.
Chemical Information
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No. CAS 916482-17-2
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Appearance Solid
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Peso molecular 407.96
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Fòrmula C20H26ClN3O2S
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Color White to off-white
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SMILES
CCCCCCC(SC1=NC(NC2=CC=CC(C)=C2C)=CC(Cl)=N1)C(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : 125 mg/mL (306.40 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Koeberle A, et al. The molecular pharmacology and in vivo activity of 2-(4-chloro-6-(2,3-dimethylphenylamino)pyrimidin-2-ylthio)octanoic acid (YS121), a dual inhibitor of microsomal prostaglandin E2 synthase-1 and 5-lipoxygenase. J Pharmacol Exp Ther. 2010 Mar;332(3):840-8. [Content Brief]
[3]. Rau O, et al. Alpha-alkyl substituted pirinixic acid derivatives as potent dual agonists of the peroxisome proliferator activated receptor alpha and gamma. Arch Pharm (Weinheim). 2008 Mar;341(3):191-5. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4512 mL | 12.2561 mL | 24.5122 mL | 61.2805 mL |
| 5 mM | 0.4902 mL | 2.4512 mL | 4.9024 mL | 12.2561 mL | |
| 10 mM | 0.2451 mL | 1.2256 mL | 2.4512 mL | 6.1281 mL | |
| 15 mM | 0.1634 mL | 0.8171 mL | 1.6341 mL | 4.0854 mL | |
| 20 mM | 0.1226 mL | 0.6128 mL | 1.2256 mL | 3.0640 mL | |
| 25 mM | 0.0980 mL | 0.4902 mL | 0.9805 mL | 2.4512 mL | |
| 30 mM | 0.0817 mL | 0.4085 mL | 0.8171 mL | 2.0427 mL | |
| 40 mM | 0.0613 mL | 0.3064 mL | 0.6128 mL | 1.5320 mL | |
| 50 mM | 0.0490 mL | 0.2451 mL | 0.4902 mL | 1.2256 mL | |
| 60 mM | 0.0409 mL | 0.2043 mL | 0.4085 mL | 1.0213 mL | |
| 80 mM | 0.0306 mL | 0.1532 mL | 0.3064 mL | 0.7660 mL | |
| 100 mM | 0.0245 mL | 0.1226 mL | 0.2451 mL | 0.6128 mL |
YS121 Related Classifications
HY-111140 Related Classifications
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