1. Metabolic Enzyme/Protease
    Neuronal Signaling
    Autophagy
  2. FAAH
    Autophagy
  3. PF-3845

PF-3845 

Cat. No.: HY-14380 Purity: 99.90%
Handling Instructions

PF-3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 μM); showing negligible activity against FAAH2.

For research use only. We do not sell to patients.

PF-3845 Chemical Structure

PF-3845 Chemical Structure

CAS No. : 1196109-52-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
5 mg USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 840 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PF-3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 μM); showing negligible activity against FAAH2. IC50 value: 0.23 uM Target: FAAH PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile [1]. PF-3845 treated mice (10 mg/kg, i.p.) shows rapid and complete inactivation of FAAH in the brain, as judged by competitive activity-based protein profiling (ABPP) with the serine hydrolase-directed probe fluorophosphonate (FP)-rhodamine. PF-3845 shows a long duration of action up to 24 hour. PF-3845-treated mice also shows dramatic (>10-fold) elevation in brain levels of AEA and other NAEs (N-pamitoyl ethanolamine [PEA] and N-oleoyl ethanolamine [OEA]). FAAH is AEA-degrading enzyme fatty acid amide hydrolase. PF-3845 (1–30 mg/kg, oral administration [p.o.]) causes a dose dependent inhibition of mechanical allodynia with a minimum effective dose (MED) of 3 mg/kg (rats are analyzed at 4 hour post dosing with PF-3845). At higher doses (10 and 30 mg/kg), PF-3845 inhibits pain responses to an equivalent, if not greater, degree than the nonsteroidal anti-inflammatory drug naproxen (10mg/kg, p.o.) [1]. PF-3845 (10 mg/kg, i.p.) significantly reverses LPS-induced tactile allodynia, but doesn't modify paw withdrawal thresholds in the saline-injected paw [2].

Molecular Weight

456.46

Formula

C₂₄H₂₃F₃N₄O₂

CAS No.

1196109-52-0

SMILES

O=C(N1CCC(CC2=CC=CC(OC3=NC=C(C=C3)C(F)(F)F)=C2)CC1)NC4=CN=CC=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (219.08 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1908 mL 10.9539 mL 21.9077 mL
5 mM 0.4382 mL 2.1908 mL 4.3815 mL
10 mM 0.2191 mL 1.0954 mL 2.1908 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.48 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PF-3845PF3845PF 3845FAAHAutophagyFatty acid amide hydrolaseInhibitorinhibitorinhibit

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Product Name:
PF-3845
Cat. No.:
HY-14380
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