1. Membrane Transporter/Ion Channel
  2. Sodium Channel

PF-06869206 

Cat. No.: HY-112065
Handling Instructions

PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.

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

PF-06869206 Chemical Structure

PF-06869206 Chemical Structure

CAS No. : 2227425-05-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 605 In-stock
Estimated Time of Arrival: December 31
5 mg USD 550 In-stock
Estimated Time of Arrival: December 31
10 mg USD 850 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2600 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.

IC50 & Target

IC50: 380 nM (NaPi2a/SLC34A1)[1]

In Vitro

PF-06869206 shows a balance of attributes with 380 nM NaPi2a inhibition potency, excellent subtype selectivity, and acceptable aqueous solubility (46 μM). PF-06869206 is profiled for potency in the rodent NaPi2a and NaPi2c cell lines. PF-06869206 shows comparable submicromolar activity for the human, rat, and mouse NaPi2a isoforms with IC50s of 0.4±0.047 μM and 0.54±0.099 μM for rat NaPi2a and mouse NaPi2a, respectively[1].

In Vivo

PF-06869206 is evaluated in rodent PK studies to determine suitability for in vivo pharmacology exploration. Results show moderate clearance in both rat and mouse. Oral bioavailability at 5 mg/kg is good in rat and moderate in mouse. At higher oral doses of 50 mg/kg, supraproportional increases in exposure are observed in both species, suggestive of saturation of clearance. PF-06869206 has moderate terminal elimination half-life (t1/2=1.35 h, and 0.75 h for Wistar-Han rats (10 mg/kg, iv), and C57BL6 mice (1 mg/kg, iv)). Furthermore, permeability is good (14×10-6 cm/s), and rat liver microsome (RLM) clearance is low (<14 μL/min/mg; HLM=39 μL/min/mg)[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (333.56 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6684 mL 13.3422 mL 26.6845 mL
5 mM 0.5337 mL 2.6684 mL 5.3369 mL
10 mM 0.2668 mL 1.3342 mL 2.6684 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Rats and Mice[1]
Male Wistar-Han rats (n=2) are treated with PF-06869206 (1 mg/kg, 5 mg/kg, and 50 mg/kg; 2 mL/kg for iv or 10 mL/kg for po) . C57BL6 mice (n=2) are treated with PF-06869206 (1 mg/kg, 5 mg/kg, and 50 mg/kg; 2 mL/kg for iv or 10 mL/kg for po) [1].

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

References
Molecular Weight

374.75

Formula

C₁₅H₁₄ClF₃N₄O₂

CAS No.

2227425-05-8

SMILES

ClC1=C(C)NC2=C(N3C[[email protected]@H](CO)OCC3)C(C#N)=C(C(F)(F)F)N=C21

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PF-06869206
Cat. No.:
HY-112065
Quantity:

PF-06869206

Cat. No.: HY-112065