生物活性
SB-408124是一种选择性的非肽orexin OX1受体拮抗剂(人OX1和OX2受体的Kb值分别为21.7和1405 nM)。体内口服后阻断orexin-A诱导的修饰。
靶点信息
| OX1 (membrane) | OX1 (whole cell) | | | |
| 27 nM(Ki) | 57 nM(Ki) | | | |
化学数据
| 目录号 | A11567 |
| 作用机制 | Antagonist (拮抗剂) |
| M. Wt | 356.37 |
| Formula | C19H18F2N4O |
| Purity | >99% |
| Storage | Store lyophilized at -20ºC, keep desiccated.
In lyophilized form, the chemical is stable for36 months.
In solution, store at -20ºC and use within3 monthsto prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles. |
| CAS No. | 288150-92-5 |
| Synonyms | SB408124, SB 408124 |
| SMILES | CC1=NC2=C(C=C(C=C2C(=C1)NC(=O)NC3=CC=C(C=C3)N(C)C)F)F |
溶解度
| In vitro (25°C) | DMSO | 35 mg/mL (98.2 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W | 28 mg/mL |
*<1 mg/ml means slightly soluble or insoluble.
*Please note that Adooq 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. |
储备液配制
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
| 0.1 mM | 28.06 mL | 140.3 mL | 280.61 mL |
| 0.5 mM | 5.61 mL | 28.06 mL | 56.12 mL |
| 1 mM | 2.81 mL | 14.03 mL | 28.06 mL |
| 5 mM | 0.56 mL | 2.81 mL | 5.61 mL |
*The above data is based on the productmolecular weight 356.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
