I am currently working on a drug that is very sensitive to blood esterases. I am looking for a good esterase inhibitor to stop the reaction once the blood is withdrawn.
Please suggest me a good esterase inhibitor to overcome this problem?
Had anyone tried sodium fluoride (NaF)? I heard that it works better. If so, please let me know the concentration and volume of NaF per mL of blood.
I would greatly appreciate your help.
Regards
K. Eshvendar Reddy
Dear Kasala,
There are different types of esterase inhibitors that you could use to inhibit esterases. Paraoxon & ebelactone are among the most used esterase inhibitors for such cases.
Paraoxon is a parasympathomimetic which acts as an acetylcholinesterase inhibitor. It is an organophosphate oxon, and the active metabolite of the insecticide parathion. It is also used as an ophthalmological drug against glaucoma. Paraoxon is one of the most potent acetylcholinesterase-inhibiting insecticides available, around 70% as potent as the nerve agent sarin, and so is now rarely used as an insecticide due to the risk of poisoning to humans and other animals.
Ebelactone A microbial
esterase inhibitor
Synonym: 3,11- Dihydroxy- 2,4,6,8,10,12- hexamethyl- 9- oxo- 6- tetradecenoic acid 1,3-lactone
Product Literature References
Acylpeptide hydrolase: inhibitors and some active site residues of the human enzyme: A. Scaloni, et al.; J. Biol. Chem. 267, 3811 (1992), Abstract; Full Text
Biosynthetic studies of ebelactone A and B by 13C NMR spectrometry: K. Uotani, et al.; J. Antibiot. (Tokyo) 35, 1670 (1982), Abstract;
Structural studies on ebelactone A and B, esterase inhibitors produced by actinomycetes: K. Uotani, et al.; J. Antibiot. (Tokyo) 35, 1495 (1982), Abstract;
Ebelactone, an inhibitor of esterase, produced by actinomycetes: H. Umezawa, et al.; J. Antibiot. (Tokyo) 33, 1594 (1980), Abstract.
http://www.enzolifesciences.com/product-listing/?product_subtype=Inhibitor&text=Esterase&gclid=CjwKEAjw2PK7BRDPz5nDh9GjoGcSJAAybcS3zbGIfQYvCjyk9dm98N53_eKkFYigHcQHVrZBBTiaLhoCcdvw_wcB
Hoping this will be helpful,
Rafik
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