Fig. 1 · Structure

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PF-915275

11β-HSD1 inhibitor

PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells).

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
3T3-L1 EC50 23.55 μM Cytotoxicity against mouse 3T3L1 cells measured after 72 hrs by celltiter-glo luminescent cell viability assay [PMID: 31294974]
HEK293 IC50 > 500 μM Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay [PMID: 31294974]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 857290-04-1
Applications

11β-HSD1 inhibitor

Formula C18H14N4O2S
Molecular Weight 350.39
SMILES
N#CC1=CC=C(C2=CC=C(S(NC3=NC(N)=CC=C3)(=O)=O)C=C2)C=C1

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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