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

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

PF-05085727 Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • Biological Activity

  • Purity & Documentation

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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)

Cellular Effect
Cell Line Type Value Description References
Sf21 IC50
2.3 nM
Compound: 1
Inhibition of full length recombinant human PDE2A expressed in Sf21 cells using [3H]-cGMP as substrate by scintillation proximity assay
Inhibition of full length recombinant human PDE2A expressed in Sf21 cells using [3H]-cGMP as substrate by scintillation proximity assay
[PMID: 23651455]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-05085727 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

413.40

Formula

C20H18F3N7
CAS No.
Appearance

Solid

Color

White to yellow

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (151.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.60%

SDS (251 KB)

COA (255 KB) LCMS (96 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4190 mL 12.0948 mL 24.1896 mL 60.4741 mL
5 mM 0.4838 mL 2.4190 mL 4.8379 mL 12.0948 mL
10 mM 0.2419 mL 1.2095 mL 2.4190 mL 6.0474 mL
15 mM 0.1613 mL 0.8063 mL 1.6126 mL 4.0316 mL
20 mM 0.1209 mL 0.6047 mL 1.2095 mL 3.0237 mL
25 mM 0.0968 mL 0.4838 mL 0.9676 mL 2.4190 mL
30 mM 0.0806 mL 0.4032 mL 0.8063 mL 2.0158 mL
40 mM 0.0605 mL 0.3024 mL 0.6047 mL 1.5119 mL
50 mM 0.0484 mL 0.2419 mL 0.4838 mL 1.2095 mL
60 mM 0.0403 mL 0.2016 mL 0.4032 mL 1.0079 mL
80 mM 0.0302 mL 0.1512 mL 0.3024 mL 0.7559 mL
100 mM 0.0242 mL 0.1209 mL 0.2419 mL 0.6047 mL
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PF-05085727 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-050857271415637-72-7PF05085727PF 05085727Phosphodiesterase (PDE)brainpenetrantBBBcortexstriatumhippocampusTHLEcellInhibitorinhibitorinhibit

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