PF-06869206
This product is for research use only, not for human use. We do not sell to patients.
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Size | Price | Stock |
---|---|---|
250mg | $950 | Check With Us |
500mg | $1550 | Check With Us |
1g | $2325 | Check With Us |
Cat #: V4476 CAS #: 2227425-05-8 Purity ≥ 98%
Description: PF-06869206 (PF06869206) is a novel, potent, selective and orally bioavailable inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with the potential to treat CKD.
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Molecular Weight (MW) | 374.75 |
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Molecular Formula | C15H14ClF3N4O2 |
CAS No. | 2227425-05-8 |
Storage | -20℃ for 3 years in powder formr |
-80℃ for 2 years in solvent |
Protocol | 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 |
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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) |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
Solvent volume to be added | Mass (the weight of a compound) | |||
---|---|---|---|---|
Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.6684 mL | 13.3422 mL | 26.6845 mL | 53.3689 mL |
5mM | 0.5337 mL | 2.6684 mL | 5.3369 mL | 10.6738 mL |
10mM | 0.2668 mL | 1.3342 mL | 2.6684 mL | 5.3369 mL |
20mM | 0.1334 mL | 0.6671 mL | 1.3342 mL | 2.6684 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
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mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.