1313034-82-0
1313034-82-0 structure
- Name: PKM-833
- Chemical Name: PKM-833
- CAS Number: 1313034-82-0
- Molecular Formula: C19H20F3N5O2
- Molecular Weight: 407.397
- Create Date: 2022-07-01 16:45:50
- Modify Date: 2025-08-25 19:10:16
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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.
| Name | PKM-833 |
|---|
| Description | 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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| References | 1. Toshiya Endo, et al. Pharmacol Res Perspect. 2020 Apr;8(2):e00569. |
| Molecular Formula | C19H20F3N5O2 |
|---|---|
| Molecular Weight | 407.397 |