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Informacje o tej pozycji
Wzór empiryczny (zapis Hilla):
C24H23N3O5
Numer CAS:
Masa cząsteczkowa:
433.46
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality Segment
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: ≥5 mg/mL at warmed
storage temp.
−20°C
SMILES string
[O-][N+](=O)c1ccc(OC(=O)N2CCN(CC2)Cc3cccc(Oc4ccccc4)c3)cc1
InChI
1S/C24H23N3O5/c28-24(32-22-11-9-20(10-12-22)27(29)30)26-15-13-25(14-16-26)18-19-5-4-8-23(17-19)31-21-6-2-1-3-7-21/h1-12,17H,13-16,18H2
InChI key
QNYRAEKLMNDRFY-UHFFFAOYSA-N
Application
JZL195 has been used:
- as a selective inhibitor of endocannabinoid (eCB) clearance enzymes to induce in vivo long-term depression at CA3-CA1 synapses and at prelimbic (PrL)-nucleus accumbens (NAc)synapses, to study the neuroprotective action of eCB[1]
- to inhibit the action of hydrolytic enzymes that limit eCB activity, to study the effect of 2-linoleoylglycerol (2-LG) on the human CB1 receptor activity[2]
- as a dual fatty acid amide hydrolase (FAAH)/monoacylglycerol lipase (MAGL) inhibitor to study its dose-related antipruritic effect on the serotonin (5-HT)-induced scratching model[3]
Biochem/physiol Actions
JZL195 is a dual inhibitor of FAAH and MAGL.
JZL195 is a potent dual inhibitor of Monoacylglycerol lipase (MAGL) and fatty acid amide hydrolase (FAAH), enzymes that degrade the endocannabinoids 2-arachidonoylglycerol (2-AG) and anandamide (AEA), the endogenous ligands for the cannabinoid G-protein coupled receptors CB1 and CB2. IC50 values are 2 nM for MAGL and 4 nM for FAAH. JZL195 has been shown to inhibit endocannabinoid hydrolysis and elevate 2-AG and AEA levels in vivo.
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Ta pozycja | |||
|---|---|---|---|
| form powder | form powder | form powder | form powder |
| assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) | assay ≥98% (HPLC) |
| storage temp. −20°C | storage temp. 2-8°C | storage temp. 2-8°C | storage temp. 2-8°C |
| solubility DMSO: ≥5 mg/mL at warmed | solubility DMSO: 1 mg/mL, clear (warmed) | solubility DMSO: 15 mg/mL, clear | solubility DMSO: 10 mg/mL (clear solution) |
| color white to beige | color white to light brown | color white to beige | color white to beige |
| Quality Level 100 | Quality Level 100 | Quality Level 100 | Quality Level - |
Klasa składowania
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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