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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
room temp
SMILES字符串
[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 key
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
历史批次信息供参考:
Xin Yang et al.
Drug metabolism and disposition: the biological fate of chemicals, 46(7), 1023-1029 (2018-04-21)
11β-Hydroxysteroid dehydrogenase 1 (11β-HSD1) is distributed mainly in the human liver, with no detectable levels in the intestine or kidney, based on a newly developed proteomic approach. 11β-HSD1 is mostly membrane-bound and retained in the liver microsomal fraction. Interindividual variability
Se Jin Park et al.
British journal of pharmacology, 172(21), 5083-5095 (2015-08-01)
The anti-inflammatory and immunomodulatory effects of macrolides include the ability to decrease mucus secretion and inhibit inflammatory mediators in chronic rhinosinusitis. Nevertheless, their mechanisms of action remain to be determined. Here we have investigated the effects of macrolide antibiotics (clarithromycin
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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