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.
|Storage||Store at -20°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 476.05. Batch specific molecular weights may vary from batch to batch due to solvent 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||2.1 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|
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.
View Related Products by Product Action
Keywords: SR 144528, SR 144528 supplier, SR144528, high, affinity, selective, cannabinoid, receptors, CB2, inverse, agonists, orally, bioavailable, immunology, Receptors, 5039, Tocris Bioscience
3 Citations for SR 144528
Citations are publications that use Tocris products. Selected citations for SR 144528 include:
Presley et al (2015) Preclinical evaluation of SMM-189, a cannabinoid receptor 2-specific inverse agonist. J Neurosci 3 e00159 PMID: 26196013
Fu (2017) Activation of cannabinoid receptor type 2 by JWH133 alleviates bleomycin-induced pulmonary fibrosis in mice. Oncotarget 8 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 PMID: 27641813
Do you know of a great paper that uses SR 144528 from Tocris? Please let us know.
Reviews for SR 144528
There are currently no reviews for this product. Be the first to review SR 144528 and earn rewards!
Have you used SR 144528?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.