生物活性
Semagacestat (LY450139)是一种针对Aβ42，Aβ40和Aβ38的γ-分泌酶阻滞剂，IC50分别为10.9 nM，12.1 nM和12.0 nM。 Semagacestat还抑制Notch信号传导，IC50为14.1 nM。
靶点信息
| γ secretase(Aβ42) (H4 human glioma cells) | γ secretase(Aβ38) (H4 human glioma cells) | γ secretase(Aβ40) (H4 human glioma cells) | Notch (H4 human glioma cells) | |
| 10.9 nM | 12.0 nM | 12.1 nM | 14.1 nM | |
化学数据
| 目录号 | A10836 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 361.4 |
| Formula | C19H27N3O4 |
| 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. | 425386-60-3 |
| Synonyms | LY-450139 |
| SMILES | C[C@@H](C(=O)N[C@H]1C2=CC=CC=C2CCN(C1=O)C)NC(=O)[C@H](C(C)C)O |
溶解度
| In vitro (25°C) | DMSO | 66 mg/mL (182.6 mM) |
| Water | Insoluble |
| Ethanol | 38 mg/mL (105.13 mM) |
| In vivo | 0.5% methylcellulose | 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 | 27.67 mL | 138.35 mL | 276.7 mL |
| 0.5 mM | 5.53 mL | 27.67 mL | 55.34 mL |
| 1 mM | 2.77 mL | 13.84 mL | 27.67 mL |
| 5 mM | 0.55 mL | 2.77 mL | 5.53 mL |
*The above data is based on the productmolecular weight 361.4 . 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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