PF-04457845
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 | Check With Us |
| 500mg | $1250 | Check With Us |
| 1g | $1875 | Check With Us |
: Cat #: V4443 CAS #: 1020315-31-4 Purity ≥ 98%
Description: PF-04457845 (PF04457845) is a novel, highly potent and selective FAAH (fatty acid amide hydrolase) inhibitor with the potential for mananing pain and other nervous system disorders.
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- Physicochemical and Storage Information
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- Related Biological Data
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| Molecular Weight (MW) | 455.43 |
|---|---|
| Molecular Formula | C23H20F3N5O2 |
| CAS No. | 1020315-31-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| SMILES Code | O=C(N1CC/C(CC1)=C\C2=CC=CC(OC3=NC=C(C(F)(F)F)C=C3)=C2)NC4=NN=CC=C4 |
| Synonyms | PF-04457845; PF 04457845; PF04457845; PF-4457845; PF 4457845; PF4457845 |
| Protocol | In Vitro | PF-04457845 inhibits FAAH by a covalent, irreversible mechanism involving carbamylation of the active-site serine nucleophile of FAAH with high in vitro potency (kinact/Ki and IC50 values of 40300 M-1s-1 and 7.2 nM, respectively, for human FAAH). PF-04457845 has exquisite selectivity for FAAH relative to other members of the serine hydrolase superfamily as demonstrated by competitive activity-based protein profiling. PF-04457845 completely inhibits FAAH in human and mouse membrane proteomes at both 10 and 100 μM with no off targets. |
|---|---|---|
| In Vivo | Oral administration of PF-04457845 at 0.1 mg/kg results in efficacy comparable to that of naproxen at 10 mg/kg in a rat model of inflammatory pain. Oral administration of PF-04457845 causes a significant inhibition of mechanical allodynia measured after 4 h with a minimum effective dose (MED) of 0.1 mg/kg. Furthermore, at 0.1 mg/kg (p.o.), PF-04457845 inhibits the pain response to a comparable degree as the nonsteroidal anti-inflammatory drug naproxen at 10 mg/kg. |
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 | 2.1957 mL | 10.9786 mL | 21.9573 mL | 43.9145 mL |
| 5mM | 0.4391 mL | 2.1957 mL | 4.3915 mL | 8.7829 mL |
| 10mM | 0.2196 mL | 1.0979 mL | 2.1957 mL | 4.3915 mL |
| 20mM | 0.1098 mL | 0.5489 mL | 1.0979 mL | 2.1957 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing in vivo formulation:
Take
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µL
PEG300, mix and clarify, next add
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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.
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