PF-8380
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $750 | In Stock |
| 500mg | $1250 | In Stock |
| 1g | $1875 | In Stock |
: Cat #: V3378 CAS #: 1144035-53-9 Purity ≥ 98%
Description: PF-8380 is a novel, potent and specific autotaxin (ATX) inhibitor with an IC50 of 2.8 nM in isolated enzyme assay and 101 nM in human whole blood.
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| Molecular Weight (MW) | 478.33 |
|---|---|
| Molecular Formula | C22H21Cl2N3O5 |
| CAS No. | 1144035-53-9 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C(N1CCN(CCC(C2=CC=C3NC(OC3=C2)=O)=O)CC1)OCC4=CC(Cl)=CC(Cl)=C4 |
| Synonyms | PF8380; PF-8380; PF 8380 |
| Protocol | In Vitro | PF-8380 also inhibits rat autotaxin with an IC50 of 1.16 nM with FS-3 substrate. Potency of PF-8380 is maintained when using enzyme produced from fetal fibroblasts used in combination with lysophosphatidyl choline (LPC) as a substrate. In human whole blood incubated with PF-8380 for 2 h, autotaxin is inhibited with an IC50 of 101 nM. |
|---|---|---|
| In Vivo | The pharmacokinetic profile of PF-8380 is evaluated at an intravenous dose of 1 mg/kg and oral doses of 1 to 100 mg/kg out to 24 h. PF-8380 has mean clearance of 31 mL/min/kg, volume of distribution at steady state of 3.2 L/kg, and effective t1/2 of 1.2 h. Oral bioavailability is moderate, ranging from 43 to 83%. Plasma concentrations increased with single oral escalating doses, but Cmax increased at a rate that is approximately proportional to dose from 1 to 10 mg/kg and less than proportional to dose from 10 to 100 mg/kg. PF-8380 exposures estimated by area under the curve are approximately proportional to dose and linear up to 100 mg/kg. Plasma C16:0, C18:0, and C20:0 LPA levels are measured immediately after collection. Maximal reduction of LPA levels is observed by the 3 mg/kg dose at 0.5 h with all LPA returning at or above baseline at 24 . |
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 | 2.0906 mL | 10.4530 mL | 20.9061 mL | 41.8121 mL |
| 5mM | 0.4181 mL | 2.0906 mL | 4.1812 mL | 8.3624 mL |
| 10mM | 0.2091 mL | 1.0453 mL | 2.0906 mL | 4.1812 mL |
| 20mM | 0.1045 mL | 0.5227 mL | 1.0453 mL | 2.0906 mL |
The molarity calculator equation
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The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
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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
DMSO(Master liquid concentration
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.