Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H23N3O5 |
Molecular Weight | 433.4565 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[O-][N+](=O)C1=CC=C(OC(=O)N2CCN(CC3=CC=CC(OC4=CC=CC=C4)=C3)CC2)C=C1
InChI
InChIKey=QNYRAEKLMNDRFY-UHFFFAOYSA-N
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
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/19918051Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20099888 |
https://www.ncbi.nlm.nih.gov/pubmed/25869205
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19918051
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/20099888 |
https://www.ncbi.nlm.nih.gov/pubmed/25869205
JZL195 is a potent inhibitor of both fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), the primary enzymes responsible for degrading the endocannabinoids anandamide (AEA) and 2-arachidonoylglycerol (2-AG), respectively.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL3455 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20099888 |
13.0 nM [IC50] | ||
Target ID: CHEMBL5774 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20099888 |
19.0 nM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19918051
JZL195 was prepared as saline-emulphor emulsions by vortexing, sonicating, and gentle heating neat compound directly into an 18:1:1 vol/vol/vol solution of saline:ethanol:emulphor. JZL195 was administered as milky suspensions. Male C57BL/6J mice (< 6 months old, 20–28 g) were i.p. administered compound or an 18:1:1 vol/vol/vol saline: emulphor:ethanol vehicle at a volume of 10 mkl/g weight
Route of Administration:
Intraperitoneal
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19918051
CB1 receptor transfected CHO cell membranes were thawed on ice, centrifuged at 50,000 g for 10 min at 4 °C, and resuspended in Assay Buffer A (50mMTris-HCl (pH 7.4), 3mMMgCl2, 0.2mM EGTA, and 100 mM NaCl). Reactions containing 10 mkg of membrane protein were incubated for 90 min at 30 °C in Assay Buffer A containing 10 mkM GDP, 0.1 nM [35S]GTPgammaS, 0.1% BSA, and various concentrations of JZL 195.
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1210004-12-8
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JZL195
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46232606
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TP6P2HKJ54
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DTXSID401029877
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admin on Sat Dec 16 17:30:27 GMT 2023 , Edited by admin on Sat Dec 16 17:30:27 GMT 2023
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SUBSTANCE RECORD