916482-17-2 Usage
Description
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO), which are key enzymes involved in the synthesis of pro-inflammatory mediators such as prostaglandin E2 (PGE2) and leukotrienes (LTs). With its ability to effectively inhibit PGE2 and LT synthesis in both cell-free and intact cell assays, YS121 demonstrates potential as an anti-inflammatory agent.
Uses
Used in Pharmaceutical Industry:
YS121 is used as an anti-inflammatory agent for its ability to inhibit the synthesis of PGE2 and LTs, which are directly involved in inflammation, fever, and pain. Its dual inhibitory action on mPGES-1 and 5-LO makes it a promising candidate for the treatment of inflammatory conditions.
Used in Research Applications:
YS121 is used as a research tool for studying the roles of mPGES-1 and 5-LO in inflammation and related pathways. Its inhibitory effects on these enzymes allow researchers to investigate the underlying mechanisms of inflammatory processes and identify potential therapeutic targets.
Used in Drug Development:
YS121 serves as a lead compound in the development of new anti-inflammatory drugs. Its dual inhibitory action on mPGES-1 and 5-LO provides a unique approach to targeting inflammation and may lead to the discovery of more effective and safer treatments for various inflammatory disorders.
references
[1] koeberle a, zettl h, greiner c, et al. pirinixic acid derivatives as novel dual inhibitors of microsomal prostaglandin e2 synthase-1 and 5-lipoxygenase[j]. journal of medicinal chemistry, 2008, 51(24): 8068-8076.[2] mehrotra s, morimiya a, agarwal b, et al. microsomal prostaglandin e2 synthase‐1 in breast cancer: a potential target for therapy[j]. the journal of pathology, 2006, 208(3): 356-363.werz o, greiner c, koeberle a, et al. novel and potent inhibitors of 5-lipoxygenase product synthesis based on the structure of pirinixic acid[j]. journal of medicinal chemistry, 2008, 51(17): 5449-5453.koeberle a, rossi a, zettl h, 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]. journal of pharmacology and experimental therapeutics, 2010, 332(3): 840-848.
Check Digit Verification of cas no
The CAS Registry Mumber 916482-17-2 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 9,1,6,4,8 and 2 respectively; the second part has 2 digits, 1 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 916482-17:
(8*9)+(7*1)+(6*6)+(5*4)+(4*8)+(3*2)+(2*1)+(1*7)=182
182 % 10 = 2
So 916482-17-2 is a valid CAS Registry Number.
916482-17-2Relevant articles and documents
Rational design of a pirinixic acid derivative that acts as subtype-selective PPARγ modulator
Thieme, Theresa M.,Steri, Ramona,Proschak, Ewgenij,Paulke, Alexander,Schneider, Gisbert,Schubert-Zsilavecz, Manfred
supporting information; scheme or table, p. 2469 - 2473 (2010/07/16)
Peroxisome proliferator-activated receptor γ (PPARγ) is involved in glucose and lipid homeostasis. PPARγ agonists are in clinical use for the treatment of type 2 diabetes. Lately, a new class of selective PPARγ modulators (SPPARγMs) was developed, which are believed to show less side effects than full PPARγ agonists. We have previously shown that α-substitution of pirinixic acid, a moderate agonist of PPARα and PPARγ, leads to low micromolar active balanced dual agonists of PPARα and PPARγ. Herein we present modifications of pirinixic acid leading to subtype-selective PPARγ agonists and furthermore the development of a selective PPARγ modulator guided by molecular docking studies.
