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化学情報
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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| 化学式 | C24H28ClN3O |
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| 分子量 | 409.95 | CAS No. | 868273-06-7 | ||||
| Solubility (25°C)* | 体外 | DMSO | 82 mg/mL (200.02 mM) | ||||
| Water | Insoluble | ||||||
| Ethanol | Insoluble | ||||||
| 体内 （毎回新しく調製した物を用意してください） |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Org 27569は、Cannabinoid Receptorのallosteric modulatorであり、agonist affinityの増強とinverse agonist affinityの減少を特徴とするCB1 receptorの状態を誘導します。 |
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| in vitro | Org 27569 is an allosteric modulator of CB1 cannabinoid receptor. It significantly increases the binding of CB1 receptor agonist and causes a significant decrease in specific binding of CB1 receptor inverse agonist. This compound induces CB1 high affinity agonist binding, receptor internalization, and downstream ERK phosphorylation. The allosteric ligand promotes agonist binding to CB1, yet blocks the agonist-induced conformational changes in TM6. It traps the receptor in a distinct agonist-bound, but nonsignaling conformational state. |
| 特徴 | Traps the receptor in a distinct agonist-bound, but non-signaling conformational state. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Equilibrium Binding Assays. | |
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| Binding assays are performed with the CB1 receptor agonist [3H]CP 55,940 (0.7 nM) and the CB1 receptor antagonist [3H]SR 141716A (1.2 nM), 1 mg/ml BSA and 50 mM Tris buffer containing 0.1 mM EDTA and 0.5 mM MgCl2, pH 7.4, in a total assay volume of 500 μl. Binding is initiated by the addition of mouse brain membranes (30 μg). Assays are carried out at 37°C for 60 min before termination by addition of ice-cold wash buffer (50 mM Tris buffer and 1 mg/ml BSA) and vacuum filtration using a 24-well sampling manifold and Whatman GF/B glass-fiber filters that have been soaked in wash buffer at 4°C for 24 h. Each reaction tube is washed five times with a 4-ml aliquot of buffer. The filters are oven-dried for 60 min and then placed in 5 ml of scintillation fluid, and radioactivity is quantitated by liquid scintillation spectrometry. Specific binding is defined as the difference between the binding that occurred in the presence and absence of 1 μM concentrations of the corresponding unlabeled ligand and is 70 to 80% of the total binding. | ||
| 細胞アッセイ | 細胞株 | HEK293 |
| 濃度 | ~10 μM | |
| 反応時間 | 5 to 15 min | |
| 実験の流れ | Cells expressing CB1 receptors are exposed to ORG27569 (10 μM) for 5 to 15 min. For toxin treatment to abrogate Gi coupling effects, PTX is added to the medium at 5 ng/ml. Following an 18-h incubation in the presence of toxin, cells are washed twice with PBS and treated with compounds. Cells are washed with ice-cold PBS, and cell lysates are obtained by harvesting the cells with ice-cold lysis buffer (150 mM NaCl, 1.0% IGEPAL CA-630, 0.5% sodium deoxycholate, 0.1% SDS, and 50 mM Tris, pH 7.5 containing 4-(2-aminoethyl)benzenesulfonyl fluoride, pepstatin A, E-64, bestatin, leupeptin, and aprotinin as protease inhibitors). | |
参考
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Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| GPCR kinase subtype requirements for arrestin-2 and -3 translocation to the cannabinoid CB1 receptor and the consequences on G protein signalling [ Biochem Pharmacol, 2024, 224:116190] | PubMed: 38604257 |
| A Machine Learning Strategy for Drug Discovery Identifies Anti-Schistosomal Small Molecules [ ACS Infect Dis, 2021, 10.1021/acsinfecdis.0c00754] | PubMed: 33434015 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。