1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. PF-05085727

PF-05085727 

Cat. No.: HY-102050 Purity: >98.0%
Handling Instructions

PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11.

For research use only. We do not sell to patients.

PF-05085727 Chemical Structure

PF-05085727 Chemical Structure

CAS No. : 1415637-72-7

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Based on 1 publication(s) in Google Scholar

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Description

PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11[1].

IC50 & Target[1]

PDE2A

2 nM (IC50)

In Vitro

PF-05085727 shows weak activity with IC50 of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells[1].
PF-05085727 (3 μM) shows a minimal inhibition of cytochrome P450 enzymes (CYPs), inhibits 1A2, 2C8, 2C9, 2D6 and 3A4 with percentage% of 16%, 18%, 7%, 4%, and 30%, respectively[1].
PF-05085727 (10 μM) inhibits PDE1B, PDE4B, PDE7B and PDE10A with IC50 values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively[1].

In Vivo

PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain (Cbu) to unbound plasma (Cpu) of ca. 0.27 and 0.37, respectively[1].
PF-05085727 in mice leads to an acute and exposure-dependent elevation in the accumulation of bulk levels of cGMP in cortex, striatum, and hippocampus as measured by enzyme-linked immunosorbent assay[1].

Molecular Weight

413.40

Formula

C₂₀H₁₈F₃N₇

CAS No.

1415637-72-7

SMILES

CN1C2=NC=NC(N3CCC3)=C2C(C4=C(C5=CC=C(C(F)(F)F)C=C5)N(C)N=C4)=N1

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 : 62.5 mg/mL (151.19 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4190 mL 12.0948 mL 24.1896 mL
5 mM 0.4838 mL 2.4190 mL 4.8379 mL
10 mM 0.2419 mL 1.2095 mL 2.4190 mL
*Please refer to the solubility information to select the appropriate solvent.
References

Purity: >98.0%

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Keywords:

PF-05085727PF05085727PF 05085727Phosphodiesterase (PDE)brainpenetrantBBBcortexstriatumhippocampusTHLEcellInhibitorinhibitorinhibit

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