PF-05180999
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 | $939 | Check With Us |
| 500mg | $1300 | Check With Us |
| 1g | $1950 | Check With Us |
: Cat #: V4447 CAS #: 1394033-54-5 Purity ≥ 98%
Description: PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM.
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| Molecular Weight (MW) | 414.39 |
|---|---|
| Molecular Formula | C19H17F3N8 |
| CAS No. | 1394033-54-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | FC(C1=CN=C(C2=C(C3=C4C(N5CCC5)=NC=NN4C(C)=N3)C=NN2C)C=C1)(F)F |
| Synonyms | PF05180999; PF-05180999; PF 5180999; PF5180999; PF-5180999; PF 5180999; PF999; PF-999; PF 999 |
| Protocol | In Vitro | PF-05180999 is a phosphodiesterase 2A (PDE2A) inhibitor, with an IC50 of 1.6 nM. PF-05180999 binds to the rat, dog and monkey PDE2A, with Kis of 4.2, 8.4, and 5.5 nM and IC50s of 2.6, 5.2, and 3.4 nM, respectively. PF-05180999 shows weak activity against PDE, with IC50s of 2.03 μM (PDE10A1), 26.969 μM (PDE7B), 50.09 μM (PDE11A4), and >56.25 μM (PDE1B1, PDE3A1, PDE4D3, PDE5A1, PDE6 (bovine), PDE8B, PDE9A1), respectively. PF-05180999 is also a weak inducer of CYP3A4, and with no direct inhibition of human recombinant cytochrome P450 (CYP) enzymes (1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A) and no induction of CYP1A2. |
|---|---|---|
| In Vivo | PF-05180999 (Compound 30; 0.032-0.32 mg/kg mg/kg, s.c.) dramatically reduces the working memory errors produced by ketamine in a working memory radial arm maze (RAM) model in rats. PF-05180999 causes acute and exposure-dependent elevation in the accumulation of cGMP bulk levels in the cortex, striatum, and hippocampus, but with no changes in cAMP and the associated downstream phospho-cAMP response element-binding protein (p-CREB) in mice. |
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 | 2.4132 mL | 12.0659 mL | 24.1319 mL | 48.2637 mL |
| 5mM | 0.4826 mL | 2.4132 mL | 4.8264 mL | 9.6527 mL |
| 10mM | 0.2413 mL | 1.2066 mL | 2.4132 mL | 4.8264 mL |
| 20mM | 0.1207 mL | 0.6033 mL | 1.2066 mL | 2.4132 mL |
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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:
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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.