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Merck
CN

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:
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

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 (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



历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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