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Products are for research use only. Not for human use. We do not sell to patients.
(PF 04457845; PF04457845)
PF-04457845 Chemical Structure
|Product name: PF-04457845|
|Cat. No.: HY-14376|
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.
IC50 value: 7.2 nM
It has been well tolerated in human trials even at high dose ranges with no evidence for cognitive dysfunction, and has completed Phase II clinical trials for the treatment of osteoarthritis. From Wikipedia.
|M.Wt||455.43||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
10 mM in DMSO
|1 mg||5 mg||10 mg|
|1 mM||2.1957 mL||10.9786 mL||21.9573 mL|
|5 mM||0.4391 mL||2.1957 mL||4.3915 mL|
|10 mM||0.2196 mL||1.0979 mL||2.1957 mL|
|Product Name||Sponsor Only||Condition||Start Date||End Date||Phase||Last Change Date|
|PF-04457845||Pfizer Inc||Pain||30-APR-10||30-JUN-10||Phase 1||25-JUL-10|
|Pfizer Inc||Pain||31-MAY-09||31-JUL-09||Phase 1||14-JUL-09|
|Pfizer Inc||Pain||30-NOV-09||31-JAN-10||Phase 1||16-JUL-10|
|Yale University||Cannabis dependence||30-JUN-12||31-DEC-16||Phase 2||17-SEP-13|
|Pfizer Inc||28-FEB-09||31-JUL-09||Phase 1||14-SEP-13|
|Pfizer Inc||Pain||30-NOV-09||31-MAY-10||Phase 2||27-NOV-12|
. Douglas S. Johnson, Cory Stiff, Scott E. Lazerwith et al. Discovery of PF-04457845: A Highly Potent, Orally Bioavailable, and Selective Urea FAAH Inhibitor. ACS Med. Chem. Lett., 2011, 2 (2), pp 91-96
. Ahn K, Smith SE, Liimatta MB et al. Mechanistic and pharmacological characterization of PF-04457845: a highly potent and selective fatty acid amide hydrolase inhibitor that reduces inflammatory and noninflammatory pain. J Pharmacol Exp Ther. 2011 Jul;338(1):114-24.
. Li, Gai Ling; Winter, Helen; Arends, Rosalin et al. Assessment of the pharmacology and tolerability of PF-04457845, an irreversible inhibitor of fatty acid amide hydrolase-1, in healthy subjects. British Journal of Clinical Pharmacology (2012), 73(5), 706-716.
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.
JNJ-42165279 is a FAAH inhibitor with IC50 of 70 (plusmn) 8 nM and 313 (plusmn) 28 nM for hFAAH and rFAAH, respectively.
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-3845 is a selective fatty acid amide hydrolase (FAAH) inhibitor (Ki = 0.23 (mu)M); showing negligible activity against FAAH2.
URB597 is a potent, orally bioavailable FAAH inhibitor with IC50 of 4.6 nM, with no activity on other cannabinoid-related targets.