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CAY10526 (Synonyms: 1mg/ml in ethanol; 30mg/ml in DMSO & DMF)

Catalog No.GC18856

Prostaglandin E2 (PGE2) is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases.

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CAY10526 Chemical Structure

Cas No.: 938069-71-7

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1mg
$36.00
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5mg
$158.00
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10mg
$278.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

Prostaglandin E2 (PGE2) is the major PG synthesized at sites of inflammation and plays an important role in different inflammatory diseases. It acts as a mediator of pain and inflammation and promotes bone destruction. The increased synthesis of PGE2 during inflammation can be accounted for by increased expression of both cyclooxygenase-2 (COX-2) and microsomal PGE synthase-1 (mPGES-1).[1],[2],[3] CAY10526 is an inhibitor of PGE2 production through the selective modulation of mPGES-1 expression. It dose-dependently inhibits PGE2 production in lipopolysaccharide-stimulated RAW 264.7 cells with an IC50 value of 1.8 µM without any effect on COX-2 expression.[4]

Reference:
[1]. Claveau, D., Sirinyan, M., Guay, J., et al. Microsomal prostaglandin E synthase-1 is a major terminal synthase that is selectively up-regulated during cyclooxygenase-2-dependent prostaglandin E2 production in the rat adjuvant-induced arthritis model. Journal of Immunology 170, 4738-4744 (2003).
[2]. Guay, J., Bateman, K., Gordon, R., et al. Carrageenan-induced paw edema in rat elicits a predominant prostaglandin E2 (PGE2) response in the central nervous system associated with the induction of microsomal PGE2 synthase-1. The Journal of Biological Chemisty 279(23), 24866-24872 (2004).
[3]. Stichtenoth, D.O., Thorén, S., Bian, H., et al. Microsomal prostaglandin E synthase is regulated by proinflammatory cytokines and glucocorticoids in primary rheumatoid synovial cells. Journal of Immunology 167, 469-474 (2001).
[4]. Guerrero, M.D., Aquino, M., Bruno, I., et al. Synthesis and pharmacological evaluation of a selected library of new potential anti-inflammatory agents bearing the γ-hydroxybutenolide scaffold: a new class of inhibitors of prostanoid production through the selective modulation of microsomal prostaglandin E synthase-1 expression. Journal of Medicinal Chemistry 50, 2176-2184 (2007).

Chemical Properties

Cas No. 938069-71-7 SDF
Synonyms 1mg/ml in ethanol; 30mg/ml in DMSO & DMF
Chemical Name 4-(benzo[b]thiophen-2-yl)-3-bromo-5-hydroxydihydrofuran-2(3H)-one
Canonical SMILES O=C1OC(O)C(C2=CC(C=CC=C3)=C3S2)=C1Br
Formula C12H7BrO3S M.Wt 311.1
Solubility 1mg/ml in ethanol; 30mg/ml in DMSO & DMF 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

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1 mg 5 mg 10 mg
1 mM 3.2144 mL 16.072 mL 32.144 mL
5 mM 0.6429 mL 3.2144 mL 6.4288 mL
10 mM 0.3214 mL 1.6072 mL 3.2144 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.
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.

Reviews

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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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