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Products are for research use only. Not for human use. We do not sell to patients.
(PF 3845; PF3845)
PF-3845 Chemical Structure
Protease Inhibitor Cocktail
protease inhibitor cocktails are used in mammalian cell lysates or tissue extracts to increase protein stability.
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
PF-3845 selectively inhibits FAAH by carbamylating FAAH's serine nucleophile . 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.) . 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 .
|M.Wt||456.46||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥90mg/mL Water <1.2mg/mL Ethanol ≥90mg/mL
|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|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|PF-3845||Pfizer Inc||Pain||30-NOV-09||31-MAY-10||Phase 2||27-NOV-12|
|Pfizer Inc||Pain||31-MAY-09||31-JUL-09||Phase 1||14-JUL-09|
|Pfizer Inc||28-FEB-09||31-JUL-09||Phase 1||14-SEP-13|
|Pfizer Inc||Pain||30-NOV-09||31-JAN-10||Phase 1||16-JUL-10|
|Pfizer Inc||Pain||30-APR-10||30-JUN-10||Phase 1||25-JUL-10|
|Yale University||Cannabis dependence||30-JUN-12||31-DEC-16||Phase 2||17-SEP-13|
Biochanin A(Olmelin), an O-methylated isoflavone, is a natural organic compound in the class of phytochemicals known as flavonoids; inhibit FAAH with IC(50) values of 1.8/1.4/2.4 uM for mouse/Rat/Human FAAH respectively.
FAAH inhibitor 1 is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18(plusmn)8 nM.
FAAH-IN-2 is a potent FAAH(fatty acid amide hydrolase) inhibitor extracted from Patent WO/2008/100977A2.
JZL195 is a selective and efficacious dual FAAH/MAGL inhibitor with IC50 of 13 nM and 19 nM for mouse brain FAAH and MAGL respectively.
LY2183240 is a novel and highly potent blocker of anandamide uptake (IC50 = 270 pM). LY2183240 inhibits fatty acid amide hydrolase (FAAH) activity (IC50 = 12.4 nM).
PF-04457845 is a potent and exquisitely selective inhibitor of FAAH, with an IC50 of 7.2 nM, and both analgesic and antiinflammatory effects in animal studies comparable to naproxen.
URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets.
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