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Chemical Structure| 29679-58-1 Chemical Structure| 29679-58-1

Structure of Fenoprofen
CAS No.: 29679-58-1

Chemical Structure| 29679-58-1

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Fenoprofen (LILLY-53858) is a non-steroidal anti-inflammatory drug (NSAID) used to relieve symptoms of osteoarthritis and rheumatoid arthritis, including inflammation, swelling, stiffness, and joint pain. Fenoprofen also acts as an allosteric enhancer of melanocortin receptors and promotes ERK1/2 activation.

Synonyms: LILLY-53858

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Product Citations

Product Citations

Wegner, Scott A ; Kim, Hahn ; Avalos, José L ;

Abstract: Lactate transport plays a crucial role in the metabolism, microenvironment, and survival of cancer cells. However, current drugs targeting either MCT1 or MCT4, which traditionally mediate lactate import or efflux respectively, show limited efficacy beyond in vitro models. This limitation partly arises from the existence of both isoforms in certain tumors, however existing high-affinity MCT1/4 inhibitors are years away from human testing. Therefore, we conducted an optogenetic drug screen in Saccharomyces cerevisiae on a subset of the FDA-approved drug library to identify existing scaffolds that could be repurposed as monocarboxylate transporter (MCT) inhibitors. Our findings show that several existing drug classes inhibit MCT1 activity, including non-steroidal estrogens, non-steroidal anti-inflammatory drugs (NSAIDs), and natural products (in total representing approximately 1% of the total library, 78 out of 6400), with a moderate affinity (IC50 1.8–21 μM). Given the well-tolerated nature of NSAIDs, and their known anticancer properties associated with COX inhibition, we chose to further investigate their MCT1 inhibition profile. The majority of NSAIDs in our screen cluster into a single large structural grouping. Moreover, this group is predominantly comprised of FDA-approved NSAIDs, with seven exhibiting moderate MCT1 inhibition. Since these molecules form a distinct structural cluster with known NSAID MCT4 inhibitors, such as diclofenac, ketoprofen, and indomethacin, we hypothesize that these newly identified inhibitors may also inhibit both transporters. Consequently, NSAIDs as a class, and piroxicam specifically (IC50 4.4 μM), demonstrate MCT1 inhibition at theoretically relevant human dosages, suggesting immediate potential for standalone MCT inhibition or combined anticancer therapy.

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Product Details of Fenoprofen

CAS No. :29679-58-1
Formula : C15H14O3
M.W : 242.27
SMILES Code : CC(C1=CC=CC(OC2=CC=CC=C2)=C1)C(O)=O
Synonyms :
LILLY-53858
MDL No. :MFCD00072027
InChI Key :RDJGLLICXDHJDY-UHFFFAOYSA-N
Pubchem ID :3342

Safety of Fenoprofen

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Description
enoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory drug (NSAID) used primarily to alleviate symptoms associated with arthritis, including osteoarthritis and rheumatoid arthritis, such as inflammation, swelling, stiffness, and joint pain. Additionally, Fenoprofen acts as an allosteric enhancer of melanocortin receptors and promotes ERK1/2 activation[1].[2].

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.13mL

0.83mL

0.41mL

20.64mL

4.13mL

2.06mL

41.28mL

8.26mL

4.13mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

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