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PF-915275 

Cat. No.: HY-18056 Purity: 98.32%
Handling Instructions

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). 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.

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PF-915275 Chemical Structure

PF-915275 Chemical Structure

CAS No. : 857290-04-1

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10 mM * 1  mL in DMSO USD 119 In-stock
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10 mg USD 144 In-stock
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100 mg USD 1020 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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). 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[1][2][3].

IC50 & Target

Ki: 2.3 nM (11βHSD1); EC50: 15 nM (11βHSD1)[1]

In Vitro

PF-915275 is a potent inhibitor of 11βHSD1 (in vitro HEK293, EC50 of 15 nM) in this human 11βHSD1 overexpressed cell line when coincubated in the presence of 300 nM enzyme substrate. Consistent with the species differences between human and rodent observed in biochemical assays, PF-915275 is a poor inhibitor of 11βHSD1 in rat FAO hepatoma cells, with an EC50 of 14,500 nM. PF-915275 demonstrates species-dependent potency for inhibiting cellular conversion of cortisone to cortisol in dog, monkey, and human in primary hepatocytes, with activity in human hepatocytes/monkey hepatocytes/dog hepatocytes. PF-915275 does not significantly inhibit 11βHSD2 (only 1.5% inhibition when tested at 10 μM). 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[1].

In Vivo

The inhibition of either cortisone or prednisone turnover with PF-915275 yields similar EC50 values to that in human hepatocytes (EC50 by PF-915275 is 18 and 13 nM using cortisone and prednisone substrates, respectively) in vivo 11βHSD1 activity[1].
PF-915275 dose-dependently inhibits 11βHSD1-mediated conversion of prednisone to prednisolone. A maximum of 87% inhibition is observed, with the highest tested dose of 3 mg/kg[1].
The half-life of PF-915275 is 22 hours in monkey[1].
PF-915275 (0.1-3 mg/kg; oral administration; for 8 hours; male cynomolgus monkeys) treatment shows a trend in dose-dependent lowering of fed plasma insulin after 8 h of dosing in these monkeys. Plasma insulin levels are significantly lowered (by 54 and 60%, respectively) at 1 and 3 mg/kg PF-915275 treatment. Plasma glucose or lipid levels are not altered with treatment[1].

Animal Model: Adult male cynomolgus monkeys (2-5 kg)[1]
Dosage: 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg
Administration: Oral administration; for 8 hours
Result: There was a trend in dose-dependent lowering of fed plasma insulin after 8 h of dosing in these monkeys. Plasma insulin levels were significantly lowered (by 54 and 60%, respectively).
Molecular Weight

350.39

Formula

C₁₈H₁₄N₄O₂S

CAS No.

857290-04-1

SMILES

N#CC1=CC=C(C2=CC=C(S(NC3=NC(N)=CC=C3)(=O)=O)C=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 31 mg/mL (88.47 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8540 mL 14.2698 mL 28.5396 mL
5 mM 0.5708 mL 2.8540 mL 5.7079 mL
10 mM 0.2854 mL 1.4270 mL 2.8540 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 0.83 mg/mL (2.37 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 0.83 mg/mL (2.37 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 0.83 mg/mL (2.37 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 98.32%

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Keywords:

PF-915275PF915275PF 915275OthersInhibitorinhibitorinhibit

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Product name:
PF-915275
Cat. No.:
HY-18056
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