生物活性
LY-411575是一种选择性的，细胞可渗透的小分子γ-secretase抑制剂。在表达APP或NΔE的HEK293细胞中IC50为0.078 nM/0.082 nM(基于膜/细胞)，也抑制Notch分裂，IC50为0.39 nM。
靶点信息
| γ secretase (membrane-based) (HEK293 cells expressing either APP or NδE) | γ secretase (cell-based) (HEK293 cells expressing either APP or NδE) | Notch S3 cleavage (HEK293 cells expressing either APP or NδE) | | |
| 0.078 nM | 0.082 nM | 0.39 nM | | |
化学数据
| 目录号 | A11176 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 479.48 |
| Formula | C26H23F2N3O4 |
| 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. | 209984-57-6 |
| Synonyms | LY411575 |
| SMILES | C[C@@H](C(=O)N[C@H]1C2=CC=CC=C2C3=CC=CC=C3N(C1=O)C)NC(=O)[C@H](C4=CC(=CC(=C4)F)F)O |
溶解度
| In vitro (25°C) | DMSO | 94 mg/mL (196.04 mM) |
| Water | Insoluble |
| Ethanol | 13 mg/mL (27.11 mM) |
| In vivo | 30% PEG400+0.5% Tween80+5% propylene glycol | 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 | 20.86 mL | 104.28 mL | 208.56 mL |
| 0.5 mM | 4.17 mL | 20.86 mL | 41.71 mL |
| 1 mM | 2.09 mL | 10.43 mL | 20.86 mL |
| 5 mM | 0.42 mL | 2.09 mL | 4.17 mL |
*The above data is based on the productmolecular weight 479.48. 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.
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