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Tocris/PF 915275/3291/50/50 mg

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货号: 3291/50

品牌: Tocris

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Description: Potent and selective 11β-hydroxysteroid dehydrogenase inhibitor

Chemical Name: N-(6-Amino-2-pyridinyl)-4'-cyano-[1,1'-biphenyl]-4-sulfonamide

Purity: ≥98% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent and selective 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor (K_i = 2.3 nM) that displays little activity at 11βHSD2 (1.5% inhibition at 10 μM). Inhibits the conversion of prednisone to prednisolone in human hepatocytes in vitro (EC₅₀ = 15 nM) and has antidiabetic activity in vivo. Orally active.

Compound Libraries

PF 915275 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	350.39
Formula	C₁₈H₁₄N₄O₂S
Storage	Store at RT
Purity	≥98% (HPLC)
CAS Number	857290-04-1
PubChem ID	23725123
InChI Key	ZESFDAKNYJQYKO-UHFFFAOYSA-N
Smiles	NC1=NC(NS(C(C=C3)=CC=C3C2=CC=C(C#N)C=C2)(=O)=O)=CC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	35.04	100

Preparing Stock Solutions

The following data is based on the product molecular weight 350.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.85 mL	14.27 mL	28.54 mL
5 mM	0.57 mL	2.85 mL	5.71 mL
10 mM	0.29 mL	1.43 mL	2.85 mL
50 mM	0.06 mL	0.29 mL	0.57 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Bhat et al (2008) 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 11β-hydroxysteroid dehydrogenase type 1 in cynomolgus monke J.Pharmacol.Exp.Ther. 324 299 PMID: 17921190

Fotsch and Wang (2008) Blockade of glucocorticoid excess at the tissue level: inhibitors of 11β-hydroxysteroid dehydrogenase type 1 as a therapy for type 2 diabetes. J.Med.Chem. 51 4851 PMID: 18652443

Courtney et al (2008) Modulation of 11β-hydroxysteroid dehydrogenase (11βHSD) activity biomarkers and pharmacokinetics of PF-00915275, a selective 11βHSD1 inhibitor. J.Clin.Endocrinol.Metab. 93 550 PMID: 17986636

Keywords: PF 915275, supplier, Potent, selective, 11β-hydroxysteroid, beta-hydroxysteroid, dehydrogenases, type, 1, 11βHSD1, 11betaHSD1, inhibitors, inhibits, PF915275, 11b-Hydroxysteroid, Dehydrogenase, 11b-Hydroxysteroid, Dehydrogenase, Tocris Bioscience

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