SR 144528

Name: SR 144528
Brand: Tocris Bioscience
SKU: 5039

Tocris Bioscience a Bio-Techne Brand

Catalog # 5039

Citations (8)

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Key Product Details

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)
Molecular Weight:	476.05

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Biological Activity for SR 144528

SR 144528 is a high affinity and selective CB₂ inverse agonist (K_i = 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
InChi Key	SUGVYNSRNKFXQM-XRHWURSXSA-N
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 for SR 144528

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.10 mL	10.50 mL	21.01 mL
5 mM	0.42 mL	2.10 mL	4.20 mL
10 mM	0.21 mL	1.05 mL	2.10 mL
50 mM	0.04 mL	0.21 mL	0.42 mL

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References for SR 144528

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

Kotsikorou 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. 2013 PMID: 23855811
Bouaboula G_i protein modulation induced by a selective inverse agonist for the peripheral cannabinoid receptor CB₂: implication for intracellular signalization cross-regulation. Mol.Pharmacol. 1999 PMID: 10051530
Rinaldi-Carmona SR 144528, the first potent and selective antagonist of the CB₂ cannabinoid receptor. J.Pharmacol.Exp.Ther. 1998 PMID: 9454810

Citations for SR 144528 (8)

Showing 1 - 8 of 8 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for SR 144528 include:

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
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
Acevedo-Canabal et al. (2019) Altered Swimming Behaviors in Zebrafish Larvae Lacking Cannabinoid Receptor 2. Cannabis Cannabinoid Res. 4:88
PMID: 31236475
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(61):103486
PMID: 29262578
Shang et al. (2016) Δ 9-Tetrahydrocannabinol Reverses TNFα-induced Increase in Airway Epithelial Cell Permeability through CB 2 Receptors Biochemical Pharmacology. 2016;
PMID: 27641813
Presley et al. (2015) Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist. J Neurosci. 3:e00159
PMID: 26196013

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