SR 144528
Chemical Name: 5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethylbicyclo[2.2.1]hept-2-yl]-1H-pyrazole-3-carboxamide
Purity: ≥98%
Biological Activity
SR 144528 is a high affinity and selective CB2 inverse agonist (Ki = 0.6 nM). Exhibits >700-fold selectivity for CB2 over CB1 receptors. Blocks the effects of CP 55,940 (Cat. No. 0949) on forskolin-sensitive adenylyl cyclase activity and MAPK in CHO cells expressing CB2 receptors. Also blocks CP 55,940-induced B-cell activation. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
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Background References
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SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
Rinaldi-Carmona et al.
J.Pharmacol.Exp.Ther., 1998;284:644 -
Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: implication for intracellular signalization cross-regulation.
Bouaboula et al.
Mol.Pharmacol., 1999;55:473 -
The importance of hydrogen bonding and aromatic stacking to the affinity and efficacy of cannabinoid receptor CB2 antagonist, 5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimeth
Kotsikorou et al.
J.Med.Chem., 2013;56:6593
Product Datasheets
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Citations for SR 144528
The citations listed below are publications that use Tocris products. Selected citations for SR 144528 include:
8 Citations: Showing 1 - 8
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Anti-Inflammatory Activity of a CB2 Selective Cannabinoid Receptor Agonist: Signaling and Cytokines Release in Blood Mononuclear Cells.
Authors: Capozzi Et al.
Molecules 2021;27:64
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Administration of Δ9-Tetrahydrocannabinol (THC) Post-Staphylococcal Enterotoxin B Exposure Protects Mice From Acute Respiratory Distress Syndrome and Toxicity.
Authors: Mohammed Et al.
Front Pharmacol 2020;11
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Altered Swimming Behaviors in Zebrafish Larvae Lacking Cannabinoid Receptor 2.
Authors: Acevedo-Canabal Et al.
Cannabis Cannabinoid Res 2019;4:88
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Role of Major Endocannabinoid-Binding Receptors during Mouse Oocyte Maturation.
Authors: Cecconi Et al.
Int J Mol Sci 2019;20
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Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells.
Authors: Alharris Et al.
Oncotarget 2019;10:45
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Activation of cannabinoid receptor type 2 by JWH133 alleviates bleomycin-induced pulmonary fibrosis in mice.
Authors: Fu
Oncotarget 2017;8(61):103486
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Δ 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors
Authors: Shang Et al.
Biochemical Pharmacology 2016;
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Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist.
Authors: Presley Et al.
J Neurosci 2015;3:e00159
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