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Details

Stereochemistry ACHIRAL
Molecular Formula C18H14N4O2S
Molecular Weight 350.394
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PF-915275

SMILES

NC1=CC=CC(NS(=O)(=O)C2=CC=C(C=C2)C3=CC=C(C=C3)C#N)=N1

InChI

InChIKey=ZESFDAKNYJQYKO-UHFFFAOYSA-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)

HIDE SMILES / InChI
Molecular Formula C18H14N4O2S
Molecular Weight 350.394
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800025590 | https://www.ncbi.nlm.nih.gov/pubmed/17986636

PF-915275 is a potent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (Ki = 2.3 nM) PF-915275 inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro (EC50 = 15 nM) and has antidiabetic activity in vivo. In first half 2007, Pfizer stopped developing PF 915275 for the treatment of type II diabetes mellitus.

Originator

Pfizer
420
Curator's Comment: # Pfizer

Approval Year

Unknown
149124
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Phase I
438
Unknown

Approved Use

Unknown
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
480 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
18.8 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
0.3 mg 1 times / day steady-state, oral
dose: 0.3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
61 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
202 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
956 ng/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
15 mg 1 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
7392 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
318 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
0.3 mg 1 times / day steady-state, oral
dose: 0.3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
1047 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3366 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
16344 ng × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
15 mg 1 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
23.1 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
30.4 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
0.3 mg 1 times / day steady-state, oral
dose: 0.3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
32.3 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
1 mg 1 times / day steady-state, oral
dose: 1 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
30.9 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
3 mg 1 times / day steady-state, oral
dose: 3 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
31.8 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/17986636/
15 mg 1 times / day steady-state, oral
dose: 15 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
PF-915275 plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
15 mg 1 times / day multiple, oral
Highest studied dose
Dose: 15 mg, 1 times / day
Route: oral
Route: multiple
Dose: 15 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/17986636
healthy
Health Status: healthy
Sex: M+F
Food Status: UNKNOWN
Sources:
https://pubmed.ncbi.nlm.nih.gov/17986636
Sources:
https://pubmed.ncbi.nlm.nih.gov/17986636
Sourcing

Sourcing

Vendor/AggregatorIDURL
1PlusChem LLC
1P004PLN
https://www.1pchem.com/search?query=1P004PLN
AChemBlock
P51733
http://www.achemblock.com/catalogsearch/result/?q=P51733
ApexBio Technology
B7346
https://www.apexbt.com/catalogsearch/result/?q=B7346
AstaTech
C16507
http://astatechinc.com/CPSResult.php?CRNO=C16507
BLD Pharm
BD630911
http://www.bldpharm.com/search/Search.html?keyword=BD630911
BOC Sciences
857290-04-1
http://www.bocsci.com/description.asp?cas=857290-04-1
Chem Scene
CS-5559
http://www.chemscene.com/goproductList/searchProductList?productObj=CS-5559
eMolecules
29703147
https://orderbb.emolecules.com/search/#?query=29703147
eNovation Chemicals
D621094
https://www.enovationchem.com/Products.asp?SEARCHTEXT=D621094&searchbtn.x=0&searchbtn.y=0
Exclusive Chemistry
2428
http://www.exchemistry.com/chem-catalog/product-2428.html
mcule
MCULE-6049674977
https://mcule.com/MCULE-6049674977/
MedChem Express
HY-18056
https://www.medchemexpress.com/search.html?q=HY-18056&ft=&fa=&fp=
Molnova
M16219
https://www.molnova.com/en/serch-list.html?keywords=M16219
MolPort
MolPort-023-276-737
https://www.molport.com/shop/molecule-link/MolPort-023-276-737
Tocris
3291
https://www.tocris.com/search.php?Type=QuickSearch&Value=3291
Wonderchem
WD06TNH
http://www.wonder-chem.com/search.html?text=WD06TNH
PubMed

PubMed

TitleDatePubMed
Induction of 11β-HSD 1 and activation of distinct mineralocorticoid receptor- and glucocorticoid receptor-dependent gene networks in decidualizing human endometrial stromal cells.
2013-02
Cortisol and interferon tau regulation of endometrial function and conceptus development in female sheep.
2013-02
Will treating diabetes with 11β-HSD1 inhibitors affect the HPA axis?
2010-10
N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275.
2009-07-01
Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11betaHSD1 inhibitor.
2008-02
Demonstration of proof of mechanism and pharmacokinetics and pharmacodynamic relationship with 4'-cyano-biphenyl-4-sulfonic acid (6-amino-pyridin-2-yl)-amide (PF-915275), an inhibitor of 11 -hydroxysteroid dehydrogenase type 1, in cynomolgus monkeys.
2008-01
Patents

Patents

07462634
1
20070072914
1
20110159005
1
7462634
1
8871208
1
WO2006134467A1
1

Sample Use Guides

In Vivo Use Guide
Oral dose of PF-00915275 (0.3-15 mg)
Route of Administration: Oral
In Vitro Use Guide
PF-915275 is a selective and potent inhibitor of the human 11b-HSD1 (HEK293 EC50 = 5 nM) and showed good selectivity against 11b-HSD2 (1.5% inhibition at 10 uM).
Substance Class Chemical
Created
by admin
on Mon Mar 31 21:24:42 GMT 2025
Edited
by admin
on Mon Mar 31 21:24:42 GMT 2025
Record UNII
388927163B
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PF-915275
Common Name English
N-(6-AMINOPYRIDIN-2-YL)-4'-CYANOBIPHENYL-4-SULFONAMIDE
Preferred Name English
Code System Code Type Description
PUBCHEM
23725123
Created by admin on Mon Mar 31 21:24:42 GMT 2025 , Edited by admin on Mon Mar 31 21:24:42 GMT 2025
PRIMARY
FDA UNII
388927163B
Created by admin on Mon Mar 31 21:24:42 GMT 2025 , Edited by admin on Mon Mar 31 21:24:42 GMT 2025
PRIMARY
CAS
857290-04-1
Created by admin on Mon Mar 31 21:24:42 GMT 2025 , Edited by admin on Mon Mar 31 21:24:42 GMT 2025
PRIMARY
EPA CompTox
DTXSID00235037
Created by admin on Mon Mar 31 21:24:42 GMT 2025 , Edited by admin on Mon Mar 31 21:24:42 GMT 2025
PRIMARY
NIH
NCATS
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