SR144528, peripheral CB2 receptor inverse agonist (ab146185)
Key features and details
- Potent, selective peripheral CB2 receptor inverse agonist
- CAS Number: 192703-06-3
- Purity: > 98%
Soluble in ethanol to 100 mM and in DMSO to 100 mM
- Form / State: Solid
- Source: Synthetic
Overview
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Product name
SR144528, peripheral CB2 receptor inverse agonist -
Description
Potent, selective peripheral CB2 receptor inverse agonist -
Biological description
Potent, selective peripheral CB2 receptor inverse agonist (Ki values are 0.6 and 400 nM for CB2 and CB1 receptors respectively). Decreases µ-opioid receptor expression. Enhances gastric motility in vivo.
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Purity
> 98% -
CAS Number
192703-06-3 -
Chemical structure
Properties
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Chemical name
5-(4-Chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1R,3S,4S)-2,2,4-trimethyl-3-bicyclo[2.2.1]heptanyl]pyrazole-3-carboxamide
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Molecular weight
476.05 -
Molecular formula
C29H34ClN3O -
PubChem identifier
3081355 -
Storage instructions
Store at Room Temperature. The product can be stored for up to 12 months. -
Solubility overview
Soluble in ethanol to 100 mM and in DMSO to 100 mM
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Handling
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
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SMILES
CC1=CC=C(C=C1)CN2C(=CC(=N2)C(=O)N[C@H]3[C@]4(CC[C@H](C4)C3(C)C)C)C5=CC(=C(C=C5)Cl)C -
Source
Synthetic
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Research areas
Images
Protocols
To our knowledge, customised protocols are not required for this product. Please try the standard protocols listed below and let us know how you get on.
References (7)
ab146185 has been referenced in 7 publications.
- Shalev N et al. Phytocannabinoid Compositions from Cannabis Act Synergistically with PARP1 Inhibitor against Ovarian Cancer Cells In Vitro and Affect the Wnt Signaling Pathway. Molecules 27:N/A (2022). PubMed: 36364346
- Anil SM et al. Cannabis compounds exhibit anti-inflammatory activity in vitro in COVID-19-related inflammation in lung epithelial cells and pro-inflammatory activity in macrophages. Sci Rep 11:1462 (2021). PubMed: 33446817
- Anis O et al. Cannabis-Derived Compounds Cannabichromene and ?9-Tetrahydrocannabinol Interact and Exhibit Cytotoxic Activity against Urothelial Cell Carcinoma Correlated with Inhibition of Cell Migration and Cytoskeleton Organization. Molecules 26:N/A (2021). PubMed: 33477303
- Peeri H et al. Specific Compositions of Cannabis sativa Compounds Have Cytotoxic Activity and Inhibit Motility and Colony Formation of Human Glioblastoma Cells In Vitro. Cancers (Basel) 13:N/A (2021). PubMed: 33916466
- Mazuz M et al. Synergistic cytotoxic activity of cannabinoids from cannabis sativa against cutaneous T-cell lymphoma (CTCL) in-vitro and ex-vivo. Oncotarget 11:1141-1156 (2020). PubMed: 32284791
- Nallathambi R et al. Anti-Inflammatory Activity in Colon Models Is Derived from ?9-Tetrahydrocannabinolic Acid That Interacts with Additional Compounds in Cannabis Extracts. Cannabis Cannabinoid Res 2:167-182 (2017). PubMed: 29082314
- Li MH et al. Compensatory Activation of Cannabinoid CB2 Receptor Inhibition of GABA Release in the Rostral Ventromedial Medulla in Inflammatory Pain. J Neurosci 37:626-636 (2017). Rat . PubMed: 28100744