推薦產品
品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 2 mg/mL, clear
儲存溫度
room temp
SMILES 字串
[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 密鑰
ZESFDAKNYJQYKO-UHFFFAOYSA-N
生化／生理作用
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.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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
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
Bo Wei et al.
Experimental and therapeutic medicine, 13(5), 2161-2168 (2017-06-02)
The aim of the present study was to investigate the correlation between glucocorticoid activity regulation, prostaglandin E2 (PGE2) synthesis, and synovial inflammation inhibition activity, through microsomal prostaglandin E synthase-1 (mPGES-1) expression regulated by the glucocorticoid pre-receptor regulator, 11β-hydroxysteroid dehydrogenase-1 (11β-HSD1).
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