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PKM-833

  Cat. No.:  DC70700  
Chemical Structure
1313034-82-0
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More than 5000 active chemicals with high quality for research!
Field of application
PKM-833 (PKM833) is a potent, selective, and orally active FAAH inhibitor with IC50 of 8.8 and 10 nM against human and rat FAAH, respectively.PKM‐833 showed human and rat K inact/K i values with 34 300 ± 10 800 and 128 000 ± 39 800 mol-1 L−1 s-1, respectively.PKM-833 does not inhibit human MAGL and a panel of 137 molecular targets, exhibits weak inhibitory effects (>50%) in five receptor binding assays [PFA, 5‐HT2B, sigma, Na+ channel and Cl‐ channel (GABA gated) at 20 uM.PKM-833 showed excellent brain penetration and good oral bioavailability, and elevated anandamide (AEA) concentrations in the rat brain.PKM-833 significantly attenuated formalin-induced pain responses (3 mg/kg) and improved mechanical allodynia in CFA-induced inflammatory pain (0.3-3 mg/kg) in rat models, without significant side effects on catalepsy and motor coordination up to 30 mg/kg.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1313034-82-0
Chemical Name: PKM-833
Synonyms: PKM833
Formula: C19H20F3N5O2
M.Wt: 407.397
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC10404 BIA 10-2474 BIA 10-2474 is an inhibitor of fatty acid amide hydrolase (FAAH) with IC50 values of 50 to 70mg/kg in various rat brain regions.
DC73733 UCM1341 UCM1341 (UCM 1341) is a bivalent ligand with melatonin receptor agonist (hMT1/hMT2, pKi=9.11/8.77) and fatty acid amide hydrolase (FAAH) inhibitory activity (rFAAH IC5=0.85 nM).
DC73732 ARN15381 ARN15381 is a potent, multitarget FAAH inhibitor/D3 partial agonist with low nanomolar range activity, decreases nicotine self-administration in male rats.
DC71543 Carpro-AM1 Carpro-AM1 is a dual-acting FAAH/substrate-selective COX inhibitor with an IC50 value of 94 nM for FAAH.
DC70700 PKM-833 PKM-833 (PKM833) is a potent, selective, and orally active FAAH inhibitor with IC50 of 8.8 and 10 nM against human and rat FAAH, respectively.PKM‐833 showed human and rat K inact/K i values with 34 300 ± 10 800 and 128 000 ± 39 800 mol-1 L−1 s-1, respectively.PKM-833 does not inhibit human MAGL and a panel of 137 molecular targets, exhibits weak inhibitory effects (>50%) in five receptor binding assays [PFA, 5‐HT2B, sigma, Na+ channel and Cl‐ channel (GABA gated) at 20 uM.PKM-833 showed excellent brain penetration and good oral bioavailability, and elevated anandamide (AEA) concentrations in the rat brain.PKM-833 significantly attenuated formalin-induced pain responses (3 mg/kg) and improved mechanical allodynia in CFA-induced inflammatory pain (0.3-3 mg/kg) in rat models, without significant side effects on catalepsy and motor coordination up to 30 mg/kg.
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