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Type HazMat fee for 500 gram (Estimated)
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Chemical Structure| 1196109-52-0 Chemical Structure| 1196109-52-0

Structure of PF-3845
CAS No.: 1196109-52-0

Chemical Structure| 1196109-52-0

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PF-3845 is a potent, selective and irreversible FAAH inhibitor with Ki of 230 nM, showing negligible activity against FAAH2.

Synonyms: PF-3845

4.5 *For Research Use Only !

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Product Details of PF-3845

CAS No. :1196109-52-0
Formula : C24H23F3N4O2
M.W : 456.46
SMILES Code : O=C(N1CCC(CC2=CC=CC(OC3=NC=C(C=C3)C(F)(F)F)=C2)CC1)NC4=CN=CC=C4
Synonyms :
PF-3845
MDL No. :MFCD18382105
InChI Key :NBOJHRYUGLRASX-UHFFFAOYSA-N
Pubchem ID :25154867

Safety of PF-3845

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P301+P310
Class:6.1
UN#:2811
Packing Group:

Isoform Comparison

Biological Activity

Target
  • FAAH

    FAAH, Ki:230 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Bone marrow macrophages (BMMs) 1-10 μM 4 days PF-3845 significantly inhibited RANKL-induced osteoclast differentiation, reduced the formation of TRAP-positive multinucleated cells, and decreased the expression of NFATc1 and osteoclast-specific marker genes. PMC7919013
Mouse primary astrocyte and microglia co-culture 10 µM 1 hour To assess the effect of PF-3845 on NAE levels, results showed that PF-3845 increased NAE levels. PMC8609003
Prefrontal cortex neurons 1 μM 5 minutes To evaluate the effects of PF3845 on inhibitory GABAergic neurotransmission. PF3845 significantly decreased the frequency of sIPSCs and mIPSCs, indicating it reduced GABA release via CB1R-related mechanisms. PMC8909692

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice TNBS- and DSS-induced colitis models Intraperitoneal, oral, and intracolonic administration 10 mg/kg Once or twice daily for 3 days (TNBS model) or 7 days (DSS model) To assess the anti-inflammatory action of PF-3845 and its effect on endocannabinoid and related lipid metabolism during experimental colitis. Results showed that PF-3845 exhibited significant anti-inflammatory effects in the TNBS-induced colitis model but was ineffective in the DSS model. PMC4136976
Male ICR (CD-1) mice Anxiety-like behavior model Intraperitoneal injection 1 mg/kg Two hours prior to behavioral testing PF-3845 partially prevented the anxiogenic effects of restraint stress exposure PMC5585044
Mice LPS-induced tactile allodynia model Intraperitoneal injection 1–10 mg/kg Single dose, 2 hours before testing PF-3845 reversed LPS-induced tactile allodynia by inhibiting FAAH to increase AEA levels, and the effect depended on the activation of both CB1 and CB2 receptors. PMC3423256
ICR mice Morphine-dependent mouse model Intraperitoneal injection 10 mg/kg Single administration, observed for 8 hours PF-3845 significantly attenuated a subset of spontaneous morphine withdrawal signs, including head shakes, paw flutters, and jumping behavior (only at the 6-h time point), but did not affect the incidence of diarrhea or weight loss. PMC3629394
ICR (CD-1) mice Anxiety-like behavior model Intraperitoneal injection 0.1, 1, and 10 mg/kg Single dose, 2 hours before behavioral testing PF-3845 was able to prevent restraint stress-induced anxiety in the light–dark box assay when administered before stress exposure, but had no effect under non-stressed conditions. PMC5917016
C57BL/6J female mice Experimental autoimmune encephalomyelitis (EAE) model Intraperitoneal injection 10 mg/kg Once daily, from day 3 to day 30 post immunization To evaluate the effect of FAAH inhibition on EAE, results showed that PF-3845 had no significant effect on the severity of EAE. PMC8609003
Mice Carrageenan-induced inflammatory pain model Intraperitoneal injection 1, 3, or 10 mg/kg Single administration PF-3845 significantly attenuated carrageenan-induced paw edema and mechanical allodynia. PMC3717616
C57BL/6J mice Endotoxin or cold environment-induced hypothermia model Intraperitoneal injection 10 mg/kg Single administration To evaluate the effect of PF-3845 on endotoxin or cold environment-induced hypothermia, results showed that PF-3845 had no effect on either type of hypothermia. PMC4477849
Mice FAAH(+/+) mice Intraperitoneal injection 10 mg/kg Single dose, sacrificed after 3 hours To evaluate the inhibitory effect of PF-3845 on FAAH and its impact on NAE and NAT metabolism. Results showed that PF-3845 significantly inhibited FAAH activity, leading to substantial accumulation of anandamide and other NAEs in brain, liver, and testis. PMC3023554
Mice Ligature-induced periodontitis model Intraperitoneal injection 10 mg/kg Once daily for 6 days PF-3845 significantly reduced alveolar bone loss and the number of osteoclasts in experimental periodontitis. PMC7919013

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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