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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 | C19H18F2N4O |
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分子量 | 356.37 | CAS No. | 288150-92-5 | ||||
Solubility (25°C)* | 体外 | DMSO | 36 mg/mL (101.01 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. |
製品説明 | SB408124 is a non-peptide antagonist for OX1 receptor with Ki of 57 nM and 27 nM in both whole cell and membrane, respectively, exhibits 50-fold selectivity over OX2 receptor. |
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in vitro | SB-408124 binds hypocretin type 1 receptor (HcrtR1) with pKi values of 7.57. Calcium mobilization studies shows that SB-408124 is a functional antagonist of the OX1 receptor with a affinity of approximately 50-fold selectivity over the OX2 receptor. [1] A recent study indicates that pretreatment of primary cultures of rat astrocytes with SB-401824 before Orexin A administration significantly reduced the stimulatory action of Orexin A on both basal and forskolin-acivated cAMP production. [2] |
in vivo | SB-408124 (30 μg/10 μL, administered intracerebroventricularly) decreases Orexin-A induced water intake in Wistar rats. Intracerebroventricularly administered Orexin-A (30 μg/10 μL) blocks the vasopressin (VP) level increase induced by either histamine or 2.5% NaCl administration, and this blocking effect is moderated by pretreatment with SB-408124. [3] Intracerebroventricular pretreatment with SB-408124 (50 mM, 5 μL/h) prevents Bicuculline (BIC)-induced increases in endogenous glucose production (EGP). [4] |
キナーゼアッセイ | Whole cell binding assays | |
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After overnight culture in 96-well Packard Cultur plates, the medium is discarded and cells are incubated in buffer containing 150 mM NaCl, 20 mM HEPES and 0.5% bovine serum albumin (pH 7.4) for 60 minutes at 25 °C. Saturation studies are carried out by incubating cells with a range of concentrations of [3H]SB-408124 (0.2–24 nM); the total assay volume is 250 μL. Protein content is assayed by lysing cells with 0.1M NaOH and using the Bradford method with bovine serum albumin (BSA) as a standard. Association kinetic studies are performed by measuring the specific binding of [3H]SB-408124 (3 nM) at 1–60 minutes after addition of [3H]SB-408124. All assays are terminated by washing the cells three times with 250μL ice-cold phosphate-buffered saline. A volume of 100 μL of Microscint 40 is added to each well and the plate is left at room temperature for 2 hours. Cell-associated radioactivity is then measured using a Packard Topcount, with a count time of 2 minute/well. | ||
動物実験 | 動物モデル | Male Wistar rats |
投薬量 | 30 μg/10 μL | |
投与方法 | Intracerebroventricularly (i.c.v.) injected into the lateral ventricle of the rat. |
Orphan receptor ligand discovery by pickpocketing pharmacological neighbors. [ Nat Chem Biol, 2017, 13(2):235-242] | PubMed: 27992882 |
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。