Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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5 mg | 在庫あり | ¥ 11,500 | |||
10 mg | 在庫あり | ¥ 18,500 | |||
25 mg | 在庫あり | ¥ 41,500 | |||
50 mg | 在庫あり | ¥ 74,500 | |||
100 mg | 在庫あり | ¥ 110,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 13,500 |
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. |
ターゲット&IC50 | OX1 (whole cell):57 nM(Ki), OX1 (membrane):27 nM(Ki) |
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] |
分子量 | 356.37 |
分子式 | C19H18F2N4O |
CAS No. | 288150-92-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 35.6 mg/mL (100 mM)
You can also refer to dose conversion for different animals. 詳細
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SB-408124 288150-92-5 GPCR/G Protein Neuroscience OX Receptor inhibit water membrane selectivity Inhibitor Orexin Receptor (OX Receptor) intake Hypocretin Receptor HCRT Receptor SB 408124 cell SB408124 inhibitor