SR 144528

Pricing Availability   Qty
Description: High affinity and selective CB2 inverse agonist
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% (HPLC)
Citations (13)
Literature (1)

Biological Activity for SR 144528

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 for SR 144528

M. Wt 476.05
Formula C29H34ClN3O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 192703-06-3
PubChem ID 3081355
Smiles C[C@]1(C2)[C@H](NC(C3=NN(CC4=CC=C(C)C=C4)C(C5=CC=C(Cl)C(C)=C5)=C3)=O)C(C)(C)[C@@H]2CC1

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.

Solubility Data for SR 144528

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 47.6 100
ethanol 47.6 100

Preparing Stock Solutions for SR 144528

The following data is based on the product molecular weight 476.05. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.1 mL 10.5 mL 21.01 mL
5 mM 0.42 mL 2.1 mL 4.2 mL
10 mM 0.21 mL 1.05 mL 2.1 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

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Product Datasheets for SR 144528

Certificate of Analysis / Product Datasheet
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References for SR 144528

References are publications that support the biological activity of the product.

Rinaldi-Carmona et al (1998) SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J.Pharmacol.Exp.Ther. 284 644 PMID: 9454810

Kotsikorou et al (2013) 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 J.Med.Chem. 56 6593 PMID: 23855811

Bouaboula et al (1999) Gi protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB2: implication for intracellular signalization cross-regulation. Mol.Pharmacol. 55 473 PMID: 10051530

If you know of a relevant reference for SR 144528, please let us know.

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Keywords: SR 144528, SR 144528 supplier, SR144528, high, affinity, selective, cannabinoid, receptors, CB2, inverse, agonists, orally, bioavailable, immunology, Receptors, 5039, Tocris Bioscience

13 Citations for SR 144528

Citations are publications that use Tocris products. Selected citations for SR 144528 include:

Mitzi et al (2021) Cannabinoid Receptor Activation on Haematopoietic Cells and Enterocytes Protects against Colitis. J Crohns Colitis 15 1032-1048 PMID: 33331878

Capozzi et al (2021) Anti-Inflammatory Activity of a CB2 Selective Cannabinoid Receptor Agonist: Signaling and Cytokines Release in Blood Mononuclear Cells. Molecules 27 64 PMID: 35011295

Acevedo-Canabal et al (2019) Altered Swimming Behaviors in Zebrafish Larvae Lacking Cannabinoid Receptor 2. Cannabis Cannabinoid Res 4 88 PMID: 31236475

Neta et al (2010) Cannabinoids Delta(9)-tetrahydrocannabinol and cannabidiol differentially inhibit the lipopolysaccharide-activated NF-kappaB and interferon-beta/STAT proinflammatory pathways in BV-2 microglial cells. J Biol Chem 285 1616-26 PMID: 19910459

Woong-Ki et al (2022) Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation. Respir Res 23 326 PMID: 36463179

Presley et al (2015) Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist. J Neurosci 3 e00159 PMID: 26196013

Mohammed et al (2020) Administration of Δ9-Tetrahydrocannabinol (THC) Post-Staphylococcal Enterotoxin B Exposure Protects Mice From Acute Respiratory Distress Syndrome and Toxicity. Front Pharmacol 11 PMID: 32612530

Cecconi et al (2019) Role of Major Endocannabinoid-Binding Receptors during Mouse Oocyte Maturation. Int J Mol Sci 20 PMID: 31212770

Alharris et al (2019) Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells. Oncotarget 10 45 PMID: 30713602

Fu (2017) Activation of cannabinoid receptor type 2 by JWH133 alleviates bleomycin-induced pulmonary fibrosis in mice. Oncotarget 8 103486 PMID: 29262578

Miriam et al (2020) 2-arachidonoylglycerol reduces chondroitin sulphate proteoglycan production by astrocytes and enhances oligodendrocyte differentiation under inhibitory conditions. Glia 68 1255-1273 PMID: 31894889

Manuela et al (2020) Positive Allosteric Modulation of CB1 and CB2 Cannabinoid Receptors Enhances the Neuroprotective Activity of a Dual CB1R/CB2R Orthosteric Agonist. Life (Basel) 10 PMID: 33302569

Shang et al (2016) Δ 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors Biochemical Pharmacology PMID: 27641813

Do you know of a great paper that uses SR 144528 from Tocris? Please let us know.

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Literature in this Area

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Cannabinoid Receptor Ligands Scientific Review

Cannabinoid Receptor Ligands Scientific Review

Written by Roger Pertwee, this review discusses compounds which affect the activity of the endocannabinoid system, focusing particularly on ligands that are most widely used as experimental tools and denotes compounds available from Tocris.