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PZ0400

Sigma-Aldrich

PF-915275

≥98% (HPLC)

Synonyme(s) :

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

Formule empirique (notation de Hill) :
C18H14N4O2S
Numéro CAS:
857290-04-1
Poids moléculaire :
350.39
Numéro MDL:
MFCD12828758
Code UNSPSC :
51111800
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Essai

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

room temp

Chaîne SMILES 

[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)

Clé InChI

ZESFDAKNYJQYKO-UHFFFAOYSA-N

Actions biochimiques/physiologiques

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.

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Certificats d'analyse (COA)

Lot/Batch Number

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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
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
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.
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
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