PZ0400
PF-915275
≥98% (HPLC)
别名:
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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关于此项目
经验公式（希尔记法）:
C18H14N4O2S
化学文摘社编号:
分子量:
350.39
UNSPSC Code:
51111800
NACRES:
NA.77
MDL number:
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
Quality Level
Biochem/physiol Actions
PF-915275 is an orally active, potent and selective 11beta-hydroxysteroid dehydrogenase type 1 (11β-HSD1, HSD11B1) inhibitor (human 11β-HSD1 Ki <1 nM; cellular IC50 = 5 nM using human 11β-HSD1-transfected HEK293) with reduced potency toward non-human species (human/monkey/dog hepatocytes EC50 = 20/100/120 nM; mouse 11β-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.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
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
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.
Sayaka Matsumura et al.
Dermato-endocrinology, 9(1), e1412018-e1412018 (2018-02-28)
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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