TargetMol

PF-915275

Product Code:
 
TAR-T16510
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1

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CodeSizePrice
TAR-T16510-1mg1mg£96.00
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TAR-T16510-2mg2mg£107.00
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TAR-T16510-5mg5mg£130.00
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TAR-T16510-1mL1 mL * 10 mM (in DMSO)£136.00
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TAR-T16510-10mg10mg£174.00
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TAR-T16510-25mg25mg£286.00
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TAR-T16510-50mg50mg£492.00
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TAR-T16510-100mg100mg£683.00
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TAR-T16510-500mg500mg£1,348.00
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Further Information

Bioactivity:
PF-915275 is an effective and selective inhibitor of human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1, Ki = 2.3 nM, EC50 = 15 nM in vitro HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively.
CAS:
857290-04-1
Formula:
C18H14N4O2S
Molecular Weight:
350.4
Pathway:
Metabolism
Purity:
0.9769
SMILES:
Nc1cccc(NS(=O)(=O)c2ccc(cc2)-c2ccc(cc2)C#N)n1
Target:
Dehydrogenase

References

1. Bhat BG, et al. 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. J Pharmacol Exp Ther. 2008 Jan;324(1):299-305. 2. Siu M, et al. N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11beta-hydroxysteroid dehydrogenase type 1: Discovery of PF-915275. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3493-7. 3. Courtney R, et al. Modulation of 11beta-hydroxysteroid dehydrogenase (11betaHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11betaHSD1 inhibitor. J Clin Endocrinol Metab. 2008 Feb;93(2):550-6.