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Merck

PZ0184

Sigma-Aldrich

PF-04457845

≥98% (HPLC)

Synonim(y):

N-(3-pyridazinyl)-4-(3-[5-trifluoromethyl-2-pyridinyloxy]benzylidene)piperidine-1-carboxamide, N-3-Pyridazinyl-4-[[3-[[5-(trifluoromethyl)-2-pyridinyl]oxy]phenyl]methylene]-1-piperidinecarboxamide, PF-4457845

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About This Item

Wzór empiryczny (zapis Hilla):
C23H20F3N5O2
Numer CAS:
Masa cząsteczkowa:
455.43
Numer MDL:
Kod UNSPSC:
51111800
Identyfikator substancji w PubChem:
NACRES:
NA.77

Poziom jakości

Próba

≥98% (HPLC)

Postać

powder

kolor

white to beige

rozpuszczalność

DMSO: 20 mg/mL

temp. przechowywania

room temp

ciąg SMILES

O=C(NC1=NN=CC=C1)N(CC2)CCC2=CC3=CC=CC(OC4=NC=C(C(F)(F)F)C=C4)=C3

InChI

1S/C23H20F3N5O2/c24-23(25,26)18-6-7-21(27-15-18)33-19-4-1-3-17(14-19)13-16-8-11-31(12-9-16)22(32)29-20-5-2-10-28-30-20/h1-7,10,13-15H,8-9,11-12H2,(H,29,30,32)

Klucz InChI

BATCTBJIJJEPHM-UHFFFAOYSA-N

Powiązane kategorie

Działania biochem./fizjol.

PF-04457845 is a potent, orally active, irreversible inhibitor of fatty acid amide hydrolase (FAAH), the principle enzyme involved in the degradation of the endocannabinoid anandamide. PF-04457845 is a covalent inhibitor that carbamylates FAAH′s serine nucleophile. It was shown to be both potent and selective against other serine hydrolases. It has an IC50 value of 7.2 nM for human FAAH. The endocannabinoid system is a target for therapeutic pain relief. In a rat model of inflammatory pain, PF-04457845 produced significant reduction of inflammatory pain with efficacy comparable to that of naproxen at 10 mg/kg.

Kod klasy składowania

11 - Combustible Solids

Klasa zagrożenia wodnego (WGK)

WGK 3

Temperatura zapłonu (°F)

Not applicable

Temperatura zapłonu (°C)

Not applicable


Certyfikaty analizy (CoA)

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Powiązane treści

The aim of the Cravatt research group is to understand the roles that mammalian enzymes play in physiological and pathological processes and to use this knowledge to identify novel therapeutic targets for the treatment of human disease. To achieve these goals, they develop and apply new technologies that bridge the fields of chemistry and biology, ascribing to the philosophy that the most significant biomedical problems require creative multidisciplinary approaches for their solution. The group's technological innovations address fundamental challenges in systems biology that are beyond the scope of contemporary methods. For instance, enzymes are tightly regulated by post-translational events in vivo, meaning that their activity may not correlate with expression as measured by standard genomic and proteomic approaches. Considering that it is an enzyme's activity, rather than abundance that ultimately dictates its role in cell physiology and pathology, the Cravatt group has introduced a set of proteomic technologies that directly measures this parameter. These activity-based protein profiling (ABPP) methods exploit the power of chemistry to engender new tools and assays for the global analysis of enzyme activities. The enzyme activity profiles generated by ABPP constitute unique molecular portraits of cells and tissues that illuminate how metabolic and signaling networks are regulated in vivo. Additionally, by evaluating enzymes based on functional properties rather than mere abundance, ABPP acquires high-content proteomic information that is enriched in novel markers and targets for the diagnosis and treatment of human disease.

Nasz zespół naukowców ma doświadczenie we wszystkich obszarach badań, w tym w naukach przyrodniczych, materiałoznawstwie, syntezie chemicznej, chromatografii, analityce i wielu innych dziedzinach.

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