SR144528
Based on 8 publication(s) in Google Scholar
SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.02%
- CAS No.: 192703-06-3
- Formule: C29H34ClN3O
- Masse moléculaire:476.05
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) SR144528
More- Autophagy. 2021 Nov;17(11):3592-3606. [Abstract]
- Int J Mol Sci. 2026 Feb 24;27(5):2095. [Abstract]
- Int Immunopharmacol. 2023 Oct:123:110771. [Abstract]
- ACS Omega. 2026 Apr 13;11(16):23820-23832. [Abstract]
- iScience. 2024 Jan 15;27(2):108919. [Abstract]
- J Funct Foods. 2026 May 6;141:107325.
- ACS Pharmacol Transl Sci. 2024 Feb 15;7(3):797-808. [Abstract]
- Neuroscience. 2019 Apr 15:404:246-258. [Abstract]
Customer Validation & Images
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IHC
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Flow Cytometry
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ELISA
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WB
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In Vivo Efficacy Study
Activité biologique
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CB2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
26.69 μM
Compound: SR144528
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Inverse agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as increase in NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent based cAMP Hunter assay
Inverse agonist activity at recombinant human CB2R expressed in CHOK1 cells assessed as increase in NKH477-stimulated intracellular cAMP levels after 30 mins by chemiluminescent based cAMP Hunter assay
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[PMID: 32515588] |
| HEK293 | EC50 |
23.31 nM
Compound: 1, SR144528
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Antagonist activity at CB2 receptor in HEK293 cells assessed as increase in CP-55,940 EC50 measuring inhibition of forskolin-stimulated cAMP accumulation at 1 uM incubated 20 mins prior to CP-55,940 addition measured after 7 mins by spectrophotometry (Rvb
Antagonist activity at CB2 receptor in HEK293 cells assessed as increase in CP-55,940 EC50 measuring inhibition of forskolin-stimulated cAMP accumulation at 1 uM incubated 20 mins prior to CP-55,940 addition measured after 7 mins by spectrophotometry (Rvb
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[PMID: 23855811] |
| HEK293 | IC50 |
541.9 μM
Compound: SR144528
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Displacement of 3[H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cell membranes measured after 90 mins
Displacement of 3[H]-CP55940 from human recombinant CB1 receptor expressed in HEK293 cell membranes measured after 90 mins
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[PMID: 31185414] |
| HEK293 | IC50 |
7.16 μM
Compound: SR144528
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Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins
Displacement of 3[H]-CP55940 from human recombinant CB2 receptor expressed in HEK293 cell membranes measured after 90 mins
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[PMID: 31185414] |
| HEK293 | IC50 |
96.2 nM
Compound: SR144528
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Inverse agonist activity at human CB2 receptor expressed in HEK293 EBNA cell membranes after 30 mins by [35S]-GTPgammaS binding assay
Inverse agonist activity at human CB2 receptor expressed in HEK293 EBNA cell membranes after 30 mins by [35S]-GTPgammaS binding assay
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[PMID: 28088085] |
SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM. SR144528 alone is able to stimulate in a concentration-dependent manner (EC50=26±6 nM, two experiments) the forskolin-sensitive adenylyl cyclase activity in CHO-CB2 cells with a maximum effect at 1 μM (4-fold stimulation) whereas at this concentration it has no significant effect on CHO-CB1 cells (15% inhibition)[1]. Raw 264.7 macrophages supplemented with SR144528 display reduced caspase-3 activity. SR144528 inhibits microsomal acyl-coenzymeA:cholesterol acyltransferase (ACAT) activity in a concentration-dependent manner with an IC50 value of 3.6±1.1 μM. At 10 μM, SR144528 inhibits ACAT activities ~68%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 192703-06-3
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Appearance Solid
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Masse moléculaire 476.05
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Formule C29H34ClN3O
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Color White to light yellow
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SMILES
O=C(C1=NN(CC2=CC=C(C)C=C2)C(C3=CC=C(Cl)C(C)=C3)=C1)N[C@H]4[C@@](C5)(C)CC[C@@]5([H])C4(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Autophagy
Cannabidiol inhibits human glioma by induction of lethal mitophagy through activating TRPV4. [Abstract]2021 Nov;17(11):3592-3606. PMID: 33629929 -
Int J Mol Sci
Genetically Encoded CB2R-Based Fluorescent Sensor Enables Rapid Screening and Functional Assessment of Cannabinoid Modulators. [Abstract]2026 Feb 24;27(5):2095. PMID: 41828327 -
Int Immunopharmacol
Cannabinoid receptor 2 alleviates sepsis-associated acute lung injury by modulating maturation of dendritic cells. [Abstract]2023 Oct:123:110771. PMID: 37582314 -
ACS Omega
Receptor-Selective Modulation of Cannabinoid Signaling by Cardamonin: Integrating Molecular Dynamics, Free Energy Calculations, and Behavioral Validation. [Abstract]2026 Apr 13;11(16):23820-23832. PMID: 42077871 -
iScience
Inhibition of cannabinoid degradation enhances hippocampal contextual fear memory and exhibits anxiolytic effects. [Abstract]2024 Jan 15;27(2):108919. PMID: 38318362
SR144528 purchased from MedChemExpress. Usage Cited in: iScience. 2024 Jan 15;27(2):108919. [Abstract]
Immunohistochemical analysis of CNR2 level in lung tissue from 10% DMSO, Hu308 and SR144528 (2.5 mg/kg; i.p.) group with or without LPS treatment. The immunohistochemical results revealed that CNR2 expression level was decreased in lung tissues with LPS treatment, and the decrease in CNR2 expression was reversed by Hu308 treatment, but that was obviously attenuated by SR144528 treatment. The magnification is × 100 or × 200. Scale bars, 200 or 100 μm.
SR144528 purchased from MedChemExpress. Usage Cited in: iScience. 2024 Jan 15;27(2):108919. [Abstract]
Flow cytometry analyses of CNR2 level in DCs form 10% DMSO, Hu308 and SR144528 (2.5 mg/kg; i.p.) group with or without LPS treatment. The results demonstrated that SR144528 downregulated the increased CNR2 expression in LPS-induced SA-ALI mouse models.
SR144528 purchased from MedChemExpress. Usage Cited in: iScience. 2024 Jan 15;27(2):108919. [Abstract]
CNR2 suppressed the secretion of TNF-a, IL-1β, IL-6, IL-12, IL-18 and MCP-1 of bronchoalveolar lavage fluid from form 10% DMSO, Hu308 and SR144528 (2.5 mg/kg; i.p.) group with or without LPS treatment.
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ACS Pharmacol Transl Sci
Linderane Attenuates Complete Freund's Adjuvant-Induced Pain and Anxiety in Mice by Restoring Anterior Cingulate Cortex Microglia M2 Polarization through Activating Cannabinoid 2 Receptor. [Abstract]2024 Feb 15;7(3):797-808. PMID: 38481693
SR144528 purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2024 Feb 15;7(3):797-808. [Abstract]
Western blot detection of iNOS and Arg-1 protein expression in BV2 cells. The results showed that SR144528 (10 μM; 24 h) reversed the LDR-induced upregulation of iNOS expression and downregulation of Arg-1 expression, suggesting that LDR may promote microglial polarization from the M1 state to the M2 state by activating CB2R. Antagonizing CB2R partially attenuated the analgesic and anxiolytic effects of LDR.
SR144528 purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2024 Feb 15;7(3):797-808. [Abstract]
Mechanical pain threshold and thermal pain threshold in mice after CFA injection; swelling thickness of mouse paws after CFA injection was measured. The results showed that SR144528 (SR, 3 mg/kg; i.p.; single dose, administered 30 min prior to LDR treatment) attenuated the analgesic effect of Linderane (LDR, 50 mg/kg) in mice with CFA-induced inflammatory pain by antagonizing CB2R.
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Neuroscience
Divergent Response to Cannabinoid Receptor Stimulation in High and Low Stress-Induced Analgesia Mouse Lines Is Associated with Differential G-Protein Activation. [Abstract]2019 Apr 15:404:246-258. PMID: 30794845
Solvant et solubilité
DMSO : 100 mg/mL (210.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
MAP kinase activity is measured. Briefly, cells grown to 80% confluence are maintained in culture medium containing 0.5% foetal calf serum for 24 hour prior to the application of ligands. CHO-CB1 or -CB2 cells previously washed with PBS are incubated at 37°C in the absence (basal activity) or in the presence of SR144528 (10-9 to 3×10-6 M) for 20 min. Cells are then washed at 4°C with 0.5 mL of buffer A [50 mM Tris-HCl, pH 7.5, 150 mM NaCl, 1 mM ethyleneglycol-bis-(β-aminoethyl ether) N,N,N′,N-tetraacetic acid, 1 mM Na3PO4] and lysed for 15 min in buffer A supplemented with 1% triton X-100, 10 μg/mL aprotinin, 10 μg/mL, leupeptin, 1 mM dithiothreitol and 1 mM phenylmethylsulfonyl fluoride. The solubilized cell extracts are then clarified by centrifugation at 14,000× g for 15 min at 4°C. Aliquots (15 μL) are removed and stored at -80°C until use. Phosphorylation assays are carried out at 30°C for 30 min (linear assay conditions) with γ-[33P]ATP by using the p42/p44 MAP kinase enzyme system. The radioactivity incorporated is determined by liquid scintillation counting[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
cAMP accumulations are carried out in CHO-CB1 or -CB2 cells. Cells are washed with phosphate-buffered saline (PBS) and incubated for 15 min at 37°C in 1 mL of PBS in the absence or in the presence of SR144528 (3×10-9 to 10-5M). Forskolin (3 μM final concentration) is added and cells are incubated for another 20 min at 37°C. The reaction is terminated by rapid aspiration of the assay medium and addition of 1.5 mL of ice-cold 50 mM Tris-HCl, pH 8, 4 mM ethylenediaminetetraacetic acid. Dishes are placed on ice for 5 min and then the extracts are transferred to a glass tube. Extracts are boiled and centrifuged for 10 min at 3500 g to eliminate cell debris. Aliquots from supernatant are dried and the cAMP concentration is determined by radioimmunoassay by using the scintillant proximity assay system. The basal activity is determined in the absence of forskolin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Male Wistar rats (240 to 300 g) are used in this study. One week after the animals arrived at the laboratory, three different sets of experiments are carried out. In the third set of experiments, SR144528 (1 mg/kg i.p.) is administered in rats. The effect of SR144528 is also analyzed in vehicle-treated rats. SR144528 volume is adjusted to a maximum of 4 to 5 mL/kg[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (284 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Rinaldi-Carmona M, et al. SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor. J Pharmacol Exp Ther. 1998 Feb;284(2):644-50. [Content Brief]
[2]. Thewke D, et al. AM-251 and SR144528 are acyl CoA:cholesterol acyltransferase inhibitors. Biochem Biophys Res Commun. 2009 Apr 3;381(2):181-6. [Content Brief]
[3]. Abalo R, et al. The cannabinoid antagonist SR144528 enhances the acute effect of WIN 55,212-2 on gastrointestinal motility in the rat. Neurogastroenterol Motil. 2010 Jun;22(6):694-e206. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.1006 mL | 10.5031 mL | 21.0062 mL | 52.5155 mL |
| 5 mM | 0.4201 mL | 2.1006 mL | 4.2012 mL | 10.5031 mL | |
| 10 mM | 0.2101 mL | 1.0503 mL | 2.1006 mL | 5.2515 mL | |
| 15 mM | 0.1400 mL | 0.7002 mL | 1.4004 mL | 3.5010 mL | |
| 20 mM | 0.1050 mL | 0.5252 mL | 1.0503 mL | 2.6258 mL | |
| 25 mM | 0.0840 mL | 0.4201 mL | 0.8402 mL | 2.1006 mL | |
| 30 mM | 0.0700 mL | 0.3501 mL | 0.7002 mL | 1.7505 mL | |
| 40 mM | 0.0525 mL | 0.2626 mL | 0.5252 mL | 1.3129 mL | |
| 50 mM | 0.0420 mL | 0.2101 mL | 0.4201 mL | 1.0503 mL | |
| 60 mM | 0.0350 mL | 0.1751 mL | 0.3501 mL | 0.8753 mL | |
| 80 mM | 0.0263 mL | 0.1313 mL | 0.2626 mL | 0.6564 mL | |
| 100 mM | 0.0210 mL | 0.1050 mL | 0.2101 mL | 0.5252 mL |
SR144528 Related Classifications
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