Pyromeconic acid
Pyromeconic acid and derivatives thereof are potent inhibitors of endonuclease, it shows siderophile activity.
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Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to
24 months(2-8C).
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable for up to two weeks. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please email to: service@chemfaces.com
The packaging of the product may have turned upside down during transportation, resulting in the natural compounds adhering to the neck or cap of the vial. take the vial out of its packaging and gently shake to let the compounds fall to the bottom of the vial. for liquid products, centrifuge at 200-500 RPM to gather the liquid at the bottom of the vial. try to avoid loss or contamination during handling.
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J Med Chem. 2016 Jul 14;59(13):6444-54.
Fragment-Based Identification of Influenza Endonuclease Inhibitors.[Pubmed:
27291165 ]
The influenza virus is responsible for millions of cases of severe illness annually. Yearly variance in the effectiveness of vaccination, coupled with emerging drug resistance, necessitates the development of new drugs to treat influenza infections. One attractive target is the RNA-dependent RNA polymerase PA subunit.
METHODS AND RESULTS:
Herein we report the development of inhibitors of influenza PA endonuclease derived from lead compounds identified from a metal-binding pharmacophore (MBP) library screen. Pyromeconic acid and derivatives thereof were found to be potent inhibitors of endonuclease. Guided by modeling and previously reported structural data, several sublibraries of molecules were elaborated from the MBP hits. Structure-activity relationships were established, and more potent molecules were designed and synthesized using fragment growth and fragment merging strategies.
CONCLUSIONS:
This approach ultimately resulted in the development of a lead compound with an IC50 value of 14 nM, which displayed an EC50 value of 2.1 μM against H1N1 influenza virus in MDCK cells.
Biosci Biotechnol Biochem. 1995 May;59(5):886-90.
Pyromeconic acid and its glucosidic derivatives from leaves of Erigeron annuus, and the siderophile activity of pyromeconic acid.[Pubmed:
7787303]
3'-O-Caffeylerigeroside (Pyromeconic acid 3-O-beta-D-glucoside 3'-O-caffeyl ester) was obtained from the leaves of Erigeron annuus as a new Pyromeconic acid derivative, and its structure was elucidated. Together with the gamma-pyrone derivative, Pyromeconic acid (3-hydroxy-4H-pyran-4-one) and its beta-glucoside (erigeroside) were also isolated from the aerial parts of E. annuus. The siderophile activity of Pyromeconic acid was also studied.
