Drug intelligence / Profile preview

oleoyl-estrone

Development stage
Discontinued
Lead developer
Manhattan Pharmaceuticals
Modality
Small Molecules
01

Overview

Oleoyl-estrone is a naturally occurring fatty acid ester of estrone, found in the plasma and adipose tissue of animals and humans. It has been investigated as an anti-obesity agent due to its ability in animal studies to promote loss of body fat while preserving lean body mass and maintaining nitrogen balance. Mechanistically, it acts both centrally—by resetting the hypothalamic "ponderostat" (the brain's food control center) to reduce appetite and energy intake—and peripherally—by reducing fat storage in white adipose tissue and promoting skeletal muscle utilization of fat for energy. Oleoyl-estrone also appears to spare protein stores during weight loss, maintain glycemia with lower insulin levels, increase cholesterol catabolism, inhibit lipid synthesis in adipose tissue, and inhibit 17β-hydroxysteroid dehydrogenase (reducing β‑estradiol and testosterone synthesis). Clinical trials have not demonstrated significant efficacy for weight loss compared to placebo[1][2][5][7][8][10].

Other names
oleoyl estroneoleoylestroneMerlin-2Merlin2Merlin 2Estrone 3-oleateEstrone3-oleateEstrone-3-oleateEstrone monooleateEstrone oleic acid ester
02

Targets

MC4R (Melanocortin 4 receptor)HSD17B2 (17β-HSD2 / HSD17B2)

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