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CAY10678 (Synonyms: mPGES-1 Inhibitor III)

Katalog-Nr.GC18904

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.

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CAY10678 Chemische Struktur

Cas No.: 1268709-57-4

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1mg
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5mg
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10mg
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25mg
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Sample solution is provided at 25 µL, 10mM.

Description of CAY10678

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2. Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α. CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 uM, respectively). It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration. CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β. It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.

Chemical Properties of CAY10678

Cas No. 1268709-57-4 SDF
Überlieferungen mPGES-1 Inhibitor III
Chemical Name N-cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide
Canonical SMILES O=C(C1CCN(C2=NC3=CC(C)=C(C)C=C3N2C(C)C)CC1)NC4CCCC4
Formula C23H34N4O M.Wt 382.5
Löslichkeit DMF: 15 mg/ml,DMSO: 5 mg/ml,Ethanol: 25 mg/ml,Ethanol:PBS (pH 7.2) (1:8): 0.1 mg/ml 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.

Complete Stock Solution Preparation Table of CAY10678

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.6144 mL 13.0719 mL 26.1438 mL
5 mM 0.5229 mL 2.6144 mL 5.2288 mL
10 mM 0.2614 mL 1.3072 mL 2.6144 mL
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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.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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