| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
CAY10526 selectively targets mPGES-1, the terminal enzyme in the inducible pathway of prostaglandin E2 (PGE2) synthesis. By inhibiting this enzyme, it reduces PGE2 production, a key inflammatory mediator, while potentially avoiding the gastrointestinal and cardiovascular side effects associated with COX inhibition.
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|---|---|
| ln Vitro |
In vitro, CAY10526 dose-dependently inhibits PGE2 production in lipopolysaccharide (LPS)-stimulated RAW 264.7 macrophages with an IC50 of 1.8 µM. It does not affect COX-2 expression, highlighting its selectivity.
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| ln Vivo |
In vivo, CAY10526 significantly suppresses tumor growth and increases apoptosis in melanoma xenografts. This suggests that inhibiting mPGES-1 and PGE2 production has antitumor effects, likely by modulating the tumor microenvironment.
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| Enzyme Assay |
The in vitro enzyme assay measures the inhibition of mPGES-1 activity. This is typically performed using a cell-free system where the enzyme is incubated with its substrate, prostaglandin H2 (PGH2), and the inhibitor, and the production of PGE2 is measured by ELISA or mass spectrometry.
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| Cell Assay |
In vitro cell-based assays are performed in LPS-stimulated RAW 264.7 macrophages. Cells are treated with CAY10526, and the production of PGE2 in the culture supernatant is measured by ELISA. COX-2 expression is also assessed by Western blotting to confirm the compound's selectivity.
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| Animal Protocol |
In vivo activity is evaluated in mouse xenograft models of melanoma. Tumor-bearing mice are treated with CAY10526, and tumor growth is monitored. The effect on apoptosis in tumor tissue is assessed by TUNEL staining or measuring caspase activity.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CAY10526 are not detailed in the literature. As a research compound, its primary use is in vitro and in preclinical models. Its solubility in organic solvents like ethanol and DMSO has been noted.
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| Toxicity/Toxicokinetics |
Toxicological data for CAY10526 is not available. As a research compound, it is not intended for human use. Its safety profile would need to be established if it were to be developed for therapeutic applications.
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| References | |
| Additional Infomation |
CAY10526 is a valuable research tool for studying the role of mPGES-1 and PGE2 in inflammation and cancer. Its selectivity for mPGES-1 over COX-2 makes it a useful compound for dissecting the specific contributions of the inducible PGE2 synthesis pathway. It is not an approved drug.
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| Molecular Formula |
C12H7BRO3S
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|---|---|
| Molecular Weight |
311.14
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| Exact Mass |
309.929
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| CAS # |
938069-71-7
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| PubChem CID |
16220835
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| Appearance |
Off-white to yellow solid powder
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| Density |
1.9±0.1 g/cm3
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| Boiling Point |
561.7±50.0 °C at 760 mmHg
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| Flash Point |
293.5±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.791
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| LogP |
2.54
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
17
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| Complexity |
382
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C=C(S2)C3=C(C(=O)OC3O)Br
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| InChi Key |
ICCDILPNCJIDAW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H7BrO3S/c13-10-9(11(14)16-12(10)15)8-5-6-3-1-2-4-7(6)17-8/h1-5,11,14H
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| Chemical Name |
3-(1-benzothiophen-2-yl)-4-bromo-2-hydroxy-2H-furan-5-one
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| Synonyms |
CAY 10526 CAY-10526 CAY10526
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~66.67 mg/mL (~214.27 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.03 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2140 mL | 16.0699 mL | 32.1399 mL | |
| 5 mM | 0.6428 mL | 3.2140 mL | 6.4280 mL | |
| 10 mM | 0.3214 mL | 1.6070 mL | 3.2140 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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