2. GPCR/G Protein Neuronal Signaling
  3. Cannabinoid Receptor
  4. SR144528

SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.

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CAS 番号 : 192703-06-3

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 113 在庫あり
Solution
10 mM * 1 mL in DMSO USD 113 在庫あり
Solid
5 mg $108 在庫あり
10 mg $192 在庫あり
25 mg $432 在庫あり
50 mg $744 在庫あり
100 mg $1320 在庫あり
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カスタマーレビュー

Based on 6 publication(s) in Google Scholar

SR144528 関連抗体

Top Publications Citing Use of Products

    SR144528 purchased from MedChemExpress. Usage Cited in: iScience. 2024 Jan 15;27(2):108919.

    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.

    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.

    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.

    SR144528 purchased from MedChemExpress. Usage Cited in: ACS Pharmacol Transl Sci. 2024 Feb 15;7(3):797-808.

    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.

    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.

    Cannabinoid Receptor アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    CB1 CB2

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    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

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    製品説明

    SR144528 is a potent and selective CB2 receptor antagonist with a Ki of 0.6 nM.

    IC50 & Target

    CB2

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO-K1 EC50
    26.69 3
    Compound: SR144528
    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
    		[PMID: 32515588]
    CHO-K1 EC50
    26.69 3
    Compound: SR144528
    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
    		[PMID: 32515588]
    HEK293 EC50
    23.31 1
    Compound: 1, SR144528
    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
    		[PMID: 23855811]
    HEK293 IC50
    541.9 3
    Compound: SR144528
    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
    		[PMID: 31185414]
    HEK293 IC50
    541.9 3
    Compound: SR144528
    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
    		[PMID: 31185414]
    HEK293 IC50
    7.16 3
    Compound: SR144528
    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
    		[PMID: 31185414]
    HEK293 EC50
    23.31 1
    Compound: 1, SR144528
    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
    		[PMID: 23855811]
    HEK293 IC50
    7.16 3
    Compound: SR144528
    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
    		[PMID: 31185414]
    HEK293 IC50
    96.2 1
    Compound: SR144528
    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
    		[PMID: 28088085]
    HEK293 IC50
    96.2 1
    Compound: SR144528
    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
    		[PMID: 28088085]
    CHO-K1 EC50
    26.69 3
    Compound: SR144528
    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
    		[PMID: 32515588]
    HEK293 EC50
    23.31 1
    Compound: 1, SR144528
    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
    		[PMID: 23855811]
    HEK293 IC50
    541.9 3
    Compound: SR144528
    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
    		[PMID: 31185414]
    HEK293 IC50
    7.16 3
    Compound: SR144528
    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
    		[PMID: 31185414]
    HEK293 IC50
    96.2 1
    Compound: SR144528
    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
    		[PMID: 28088085]
    体外実験

    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.

    SR144528 関連抗体
    体内実験

    No effect on the binding of [3H]-CP 55,940 to its specific sites in the brain is observed after either oral (up to 10 mg/kg) or i.c.v. (10 μg/animal) administration of SR144528 in mice. The occupancy by SR144528 of the spleen cannabinoid receptor is time-dependent and significant for at least 18 hours after oral administration at 3 mg/kg[1]. SR144528 does not induce any significant effect on gastrointestinal (GI) motility when given alone. SR144528 does not block but enhances delayedgastric emptying[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    476.05

    分子式

    C29H34ClN3O
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    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
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1006 mL 10.5031 mL 21.0062 mL
    5 mM 0.4201 mL 2.1006 mL 4.2012 mL
    10 mM 0.2101 mL 1.0503 mL 2.1006 mL
    View the 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.

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    濃度 （開始）

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    体内:

    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.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    純度とドキュメンテーション

    純度: 99.02%

    COA (255 KB) HNMR (266 KB) LCMS (100 KB)

    取扱説明書 (2659 KB)
    参考文献
    キナーゼ実験
    [1]

    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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    細胞実験
    [1]

    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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [3]

    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) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    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
    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
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    SR144528 Related Classifications

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    一般には略語で表示されます：C1V1 = C2V2

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      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    SR144528192703-06-3SR 144528SR-144528Cannabinoid ReceptorInhibitorinhibitorinhibit

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