MK-3168 (12C)
MK-3168 (12C) is a FAAH inhibitor with IC50 values of 1.0, 5.5, 1.7 nM for human, rhesus, rat, respectively. MK-3168 shows good brain uptake and FAAH-specific signal. 11C MK-3168 can be used as FAAH PET tracer.
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- CAS. Nr.: 1242441-26-4
- Formel: C21H21ClN4OS
- Molecular Weight:412.94
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
1 nM
Compound: 6
|
Inhibition of human FAAH expressed in CHO cell lysates assessed as arachidonyl-7-amino-4-methylcoumarin amide hydrolysis to 7-amino 4-methyl coumarin preincubated for 15 mins prior to substrate addition measured after 1 to 3 hrs by fluorescence assay
Inhibition of human FAAH expressed in CHO cell lysates assessed as arachidonyl-7-amino-4-methylcoumarin amide hydrolysis to 7-amino 4-methyl coumarin preincubated for 15 mins prior to substrate addition measured after 1 to 3 hrs by fluorescence assay
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[PMID: 24900701] |
| CHO | IC50 |
1.7 nM
Compound: 6
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Inhibition of rat FAAH expressed in CHO cell lysates assessed as arachidonyl-7-amino-4-methylcoumarin amide hydrolysis to 7-amino 4-methyl coumarin preincubated for 15 mins prior to substrate addition measured after 1 to 3 hrs by fluorescence assay
Inhibition of rat FAAH expressed in CHO cell lysates assessed as arachidonyl-7-amino-4-methylcoumarin amide hydrolysis to 7-amino 4-methyl coumarin preincubated for 15 mins prior to substrate addition measured after 1 to 3 hrs by fluorescence assay
|
[PMID: 24900701] |
| CHO | IC50 |
5.5 nM
Compound: 6
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Inhibition of rhesus monkey FAAH expressed in CHO cell lysates assessed as arachidonyl-7-amino-4-methylcoumarin amide hydrolysis to 7-amino 4-methyl coumarin preincubated for 15 mins prior to substrate addition measured after 1 to 3 hrs by fluorescence as
Inhibition of rhesus monkey FAAH expressed in CHO cell lysates assessed as arachidonyl-7-amino-4-methylcoumarin amide hydrolysis to 7-amino 4-methyl coumarin preincubated for 15 mins prior to substrate addition measured after 1 to 3 hrs by fluorescence as
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[PMID: 24900701] |
Chemical Information
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CAS. Nr. 1242441-26-4
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Molecular Weight 412.94
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Formel C21H21ClN4OS
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SMILES
ClC1=CN=C(SC2=C(C3=CC=C([C@H]4C[C@@H]4C(N(C)C)=O)C=C3)N=CN2C)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MK-3168 (12C) Related Classifications
HY-161965 Related Classifications
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