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SR 144528

Catalog #: 5039
13 Citations Datasheet / COA / SDS

Discontinued Product

5039 has been discontinued.
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SR 144528 | CAS No. 192703-06-3 | Cannabinoid R2 / CB2 Inverse Agonists
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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%

Product Details
Citations (13)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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

M.Wt:
476.05
Formula:
C29H34ClN3O
Solubility:
Soluble to 100 mM in DMSO and to 100 mM in ethanol
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
192703-06-3

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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Citations for SR 144528

The citations listed below are publications that use Tocris products. Selected citations for SR 144528 include:

13 Citations: Showing 1 - 10

  1. Activation of cannabinoid-2 receptor protects against Pseudomonas aeruginosa induced acute lung injury and inflammation.
    Authors: Woong-Ki Et al.
    Respir Res  2022;23:326
  2. 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
  3. Cannabinoid Receptor Activation on Haematopoietic Cells and Enterocytes Protects against Colitis.
    Authors: Mitzi Et al.
    J Crohns Colitis  2021;15:1032-1048
  4. 2-arachidonoylglycerol reduces chondroitin sulphate proteoglycan production by astrocytes and enhances oligodendrocyte differentiation under inhibitory conditions.
    Authors: Miriam Et al.
    Glia  2020;68:1255-1273
  5. 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
  6. Positive Allosteric Modulation of CB1 and CB2 Cannabinoid Receptors Enhances the Neuroprotective Activity of a Dual CB1R/CB2R Orthosteric Agonist.
    Authors: Manuela Et al.
    Life (Basel)  2020;10
  7. Altered Swimming Behaviors in Zebrafish Larvae Lacking Cannabinoid Receptor 2.
    Authors: Acevedo-Canabal Et al.
    Cannabis Cannabinoid Res  2019;4:88
  8. Role of Major Endocannabinoid-Binding Receptors during Mouse Oocyte Maturation.
    Authors: Cecconi Et al.
    Int J Mol Sci  2019;20
  9. Role of miRNA in the regulation of cannabidiol-mediated apoptosis in neuroblastoma cells.
    Authors: Alharris Et al.
    Oncotarget  2019;10:45
  10. 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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