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SR144528 (SR-144528; SR 144528) is a novel and potent cannabinoid (CB2) receptor or antagonist or inverse agonist with Ki of 0.6 nM and 400 nM against CB2 and CB1 receptors, respectively.
| Targets |
CB2 receptor ( Ki = 0.6 nM )
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|---|---|
| ln Vitro |
SR144528 possesses a Ki of 0.6 nM and is a strong and specific CB2 receptor clamp antagonist. Forskolin-sensitive adenylyl cyclase activity in CHO-CB2 cells can be stimulated by SR144528 alone in a concentration-dependent manner (EC50=26±6 nM, two experiments), with the largest effect at 1 μM (4-fold stimulation). It doesn't significantly affect CHO-CB1 (15% inhibition) at this cell concentration [1]. With an IC50 value of 3.6±1.1 μM, the original 264.7 giant SR144528 supplemented with SR144528 inhibits phospholiposomal phospholipidyl-CoA:phospholipidyltransferase (ACAT) activity in a concentration-regulated manner. Approximately 68% of ACAT activity is fluoresced by SR144528 at 10 μM [2].
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| ln Vivo |
SR144528 After icv (10 μg/animal) or brain (10 mg/kg) administration, no binding of [3H]-CP 55,940 to particular brain sites was seen. SR144528 After powder formulation at 3 mg/kg, spleen engagement of brain cannabinoid receptors is time-dependent and significant for at least 18 hours [1]. On its own, SR144528 has no discernible impact on gastrointestinal (GI) motility. The delayed gastric emptying that is facilitated by SR144528 is not accompanied by a burst[3].
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| Enzyme Assay |
It measures the activity of MAP kinase. In short, 24 hours before ligands are applied, cells that have reached 80% confluence are kept in culture medium containing 0.5% foetal calf serum. After being cleaned with PBS, CHO-CB1 or -CB2 cells are cultured for 20 minutes at 37°C either without SR144528 (10-9 to 3×10-6 M) or with it present. Following a 4°C wash, cells are lysed for 15 minutes 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. Buffer A contains 50 mM Tris-HCl, pH 7.5, 150 mM NaCl, 1 mM ethyleneglycol-bis-(β-aminoethyl ether) N,N,N′,N-tetraacetic acid, and 1 mM Na3PO4. The cell extracts that have been solubilized are subsequently separated using centrifugation at 14,000 x g for 15 minutes at 4°C. Before using, remove the 15 μL aliquots and store them at -80°C. Using γ-[33P]ATP and the p42/p44 MAP kinase enzyme system, phosphorylation assays are run for 30 minutes at 30°C (linear assay conditions). Through the use of liquid scintillation counting, the radioactivity incorporated is ascertained[1].
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| Cell Assay |
In CHO-CB1 or -CB2 cells, cAMP accumulations are performed. PBS is used to wash the cells, and they are then incubated for 15 minutes at 37°C in 1 mL of PBS either with or without SR144528 (3×10-9 to 10-5M) present. Next, cells are incubated for 20 minutes at 37°C with the addition of forskolin (3 μM final concentration). Once the assay medium has been quickly aspirated, 1.5 mL of ice-cold 50 mM Tris-HCl, pH 8, and 4 mM ethylenediaminetetraacetic acid are added to stop the reaction. The extracts are then moved to a glass tube after the dishes are kept on ice for five minutes. The extracts undergo boiling and a 10-minute, 3500 g centrifugation to remove any remaining cell debris. The concentration of cAMP is measured by radioimmunoassay using aliquots from the supernatant that have been dried and the scintillant proximity assay system. Without forskolin, the basal activity is calculated[1].
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| Animal Protocol |
In this study, male Wistar rats weighing between 240 and 300 grams are utilized. Three distinct sets of experiments are conducted a week after the animals were brought to the lab. Rats receive an intraperitoneal injection of SR144528 (1 mg/kg) in the third series of experiments. Rats given vehicles are also used to examine the impact of SR144528. The maximum volume for SR144528 is set at 4 to 5 mL/kg[3].
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| References |
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| Molecular Formula |
C29H34CLN3O
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|---|---|
| Molecular Weight |
476.06
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| Exact Mass |
475.24
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| Elemental Analysis |
C, 73.17; H, 7.20; Cl, 7.45; N, 8.83; O, 3.36
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| CAS # |
192703-06-3
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| Related CAS # |
192703-06-3
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| Appearance |
Solid powder
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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
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| InChi Key |
SUGVYNSRNKFXQM-XRHWURSXSA-N
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| InChi Code |
InChI=1S/C29H34ClN3O/c1-18-6-8-20(9-7-18)17-33-25(21-10-11-23(30)19(2)14-21)15-24(32-33)26(34)31-27-28(3,4)22-12-13-29(27,5)16-22/h6-11,14-15,22,27H,12-13,16-17H2,1-5H3,(H,31,34)/t22-,27-,29+/m1/s1
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| Chemical Name |
5-(4-chloro-3-methylphenyl)-1-[(4-methylphenyl)methyl]-N-[(1S,2S,4R)-1,3,3-trimethyl-2-bicyclo[2.2.1]heptanyl]pyrazole-3-carboxamide
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| Synonyms |
SR-144528; SR 144528; SR144528
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~105.0 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.25 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1006 mL | 10.5029 mL | 21.0058 mL | |
| 5 mM | 0.4201 mL | 2.1006 mL | 4.2012 mL | |
| 10 mM | 0.2101 mL | 1.0503 mL | 2.1006 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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