916482-17-2
Chemical Structure
YS121
- CAS No.: 916482-17-2
- Formula:C20H26ClN3O2S
- Molecular Weight:407.96
IUPAC Name: 2-((4-chloro-6-((2,3-dimethylphenyl)amino)pyrimidin-2-yl)thio)octanoic acid
InChIKey: HVJBWTVMRIOTEL-UHFFFAOYSA-N
SMILES: CCCCCCC(SC1=NC(NC2=CC=CC(C)=C2C)=CC(Cl)=N1)C(O)=O
Biological Activity: 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)[1]. YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells[2]. YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively)[3]. YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research[1].
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YS121 | 99.74% | 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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- [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]
- [2]. Chang HH, et al. Identification and development of mPGES-1 inhibitors: where we are at? Future Med Chem. 2011 Nov;3(15):1909-34.
- [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]
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