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Merck
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PZ0400

Sigma-Aldrich

PF-915275

≥98% (HPLC)

Sinónimos:

N-(6-Amino-2-pyridinyl)-4′-cyano[1,1′-biphenyl]-4-sulfonamide; N-(6-Aminopyridin-2-yl)-4′-cyanobiphenyl-4-sulfonamide, PF 00915275, PF 915275, PF-00915275, PF00915275, PF915275

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About This Item

Fórmula empírica (notación de Hill):
C18H14N4O2S
Número de CAS:
857290-04-1
Peso molecular:
350.39
MDL number:
MFCD12828758
UNSPSC Code:
51111800
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

room temp

SMILES string

[S](=O)(=O)(Nc3nc(ccc3)N)c1ccc(cc1)c2ccc(cc2)C#N

InChI

1S/C18H14N4O2S/c19-12-13-4-6-14(7-5-13)15-8-10-16(11-9-15)25(23,24)22-18-3-1-2-17(20)21-18/h1-11H,(H3,20,21,22)

InChI key

ZESFDAKNYJQYKO-UHFFFAOYSA-N

Biochem/physiol Actions

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

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Chunpeng Zou et al.
Oncotarget, 8(56), 96263-96275 (2017-12-10)
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.
Ling-Ling Chang et al.
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
Ling-Ling Chang et al.
BMC pharmacology & toxicology, 19(1), 45-45 (2018-07-20)
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
Jessica K Hartman et al.
Toxicology and applied pharmacology, 355, 112-126 (2018-05-22)
Rising obesity rates worldwide have socio-economic ramifications. While genetics, diet, and lack of exercise are major contributors to obesity, environmental factors may enhance susceptibility through disruption of hormone homeostasis and metabolic processes. The obesogen hypothesis contends that chemical exposure early
B Ganesh Bhat et al.
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
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