PF-915275 is an orally active, potent and selective 11beta-hydroxysteroid dehydrogenase type 1 (11ß-HSD1, HSD11B1) inhibitor (human 11ß-HSD1 Ki <1 nM; cellular IC50 = 5 nM using human 11ß-HSD1-transfected HEK293) with reduced potency toward non-human species (human/monkey/dog hepatocytes EC50 = 20/100/120 nM; mouse 11ß-HSD1 Ki = 750 nM, rat hepatoma EC50 = 14 μM). PF-915275 (0.1-3-mg/kg via nasogastric intubations) inhibits prednisone-to-prednisolone conversion in cynomolgus monkeys (by 87% with 3 mg/kg) in vivo and reduces plasma insulin increase following prednisone & resumed feeding (4 hrs post PF-915275) among overnight fasted monkeys.
Codice della classe di stoccaggio
11 - Combustible Solids
Classe di pericolosità dell'acqua (WGK)
WGK 3
Punto d’infiammabilità (°F)
Not applicable
Punto d’infiammabilità (°C)
Not applicable
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Nonylphenol (NP) is an environmental endocrine-disrupting chemical (EDC) detected in human cord blood and milk. NP exposure in developmental periods results in hyperadrenalism and increasing 11β-hydroxysteroid dehydrogenase I (11β-HSD1) activity in an adult rat model. Alleviating 11β-HSD1 activity is therefore
The Journal of pharmacology and experimental therapeutics, 324(1), 299-305 (2007-10-09)
Glucocorticoids, through activation of the glucocorticoid receptor (GR), regulate hepatic gluconeogenesis. Elevated hepatic expression and activity of 11beta-hydroxysteroid dehydrogenase type 1 (11betaHSD1) play a key role in ligand-induced activation of the GR through the production of cortisol. Evidence from genetically
11β-HSD1 has been recognized as a potential therapeutic target for type 2 diabetes. Recent studies have shown that hyperglycemia leads to activation of 11β-HSD1, increasing the intracellular glucocorticoid levels. Excess glucocorticoids may lead to the clinical manifestations of cardiac injury.
Environmental toxicology and pharmacology, 44, 1-12 (2016-04-10)
We previously observed that nonylphenol (NP) exposure during development resulted in increases in body weight and hyperadrenalism in adult male offspring. The mechanism of hyperadrenalism includes the primary activation of the adrenal gland and the conversion of inactive glucocorticoids to
The major effects of the epidermal growth factor receptor (EGFR) signalling pathway on keratinocytes are cell proliferation, cell differentiation, and wound healing. In addition to these effects, an immunosuppressive effect of EGFR signalling has been reported. However, the precise mechanism
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