YS-121 |
| Catalog No.GC17979 |
dual inhibitor of mPGES-1
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 916482-17-2
Sample solution is provided at 25 µL, 10mM.
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YS-121 is a dual inhibitor of Microsomal prostaglandin E2 synthase-1 (mPGES-1) [1].
Cyclooxygenases (COX-1 and COX-2) have been involved in catalyzing the formation of prostaglandins and related eicosanoids and play an essential role in the pathogenesis of breast cancer. Actions of COX-2 are mediated by prostaglandin E2 (PGE2). Microsomal PGES-1 (mPGES-1), the inducible form of PGES, has a marked affinity for coupling with COX-2. Expression of mPGES-1 has been observed in inflammatory conditions and cancers of the stomach, colon, lung, endometrium, and skin [2].
YS-121 inhibited the activity of mPGES-1 with an IC50 of 3.9 μM [1]. YS-121 also inhibited the activity of 5-LO with the IC50 of 4.1 μM [3]. YS-121 effectively inhibited PGE2 and LT synthesis in both cell free and intact cell assays. Intraperitoneal administration of YS-121 (1.5 mg/kg) reduced pleural levels of PGE2 and LTB4 while blocking exudate formation and leukocyte infiltration in carrageenan-induced rat pleurisy [4]. YS-121 (10 μM) showed minor effects on COX-1 and COX-2, inhibiting these enzymes 24.8% and 38%, respectively [1].
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.
| Cas No. | 916482-17-2 | SDF | |
| Chemical Name | 2-[[4-chloro-6-[(2,3-dimethylphenyl)amino]-2-pyrimidinyl]thio]-octanoic acid | ||
| Canonical SMILES | CC1=C(NC2=CC(Cl)=NC(SC(C(O)=O)CCCCCC)=N2)C=CC=C1C | ||
| Formula | C20H26ClN3O2S | M.Wt | 408 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.451 mL | 12.2549 mL | 24.5098 mL |
| 5 mM | 0.4902 mL | 2.451 mL | 4.902 mL |
| 10 mM | 0.2451 mL | 1.2255 mL | 2.451 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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