生物活性
Avelestat，也称为AZD9668，是可口服的,高度选择性neutrophil elastase (NE)抑制剂，IC50和Ki分别为12 nM和9.4 nM,其选择性超过其他丝氨酸蛋白酶至少600倍。
靶点信息
| neutrophil elastase | neutrophil elastase | | | |
| 9.4 nM(Ki) | 12 nM | | | |
化学数据
| 目录号 | A12779 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 545.5 |
| Formula | C25H22F3N5O4S |
| 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. | 848141-11-7 |
| Synonyms | AZD9668,AZD 9668,AZD-9668 |
| SMILES | CC1=C(C=C(C(=O)N1C2=CC=CC(=C2)C(F)(F)F)C(=O)NCC3=NC=C(C=C3)S(=O)(=O)C)C4=CC=NN4C |
溶解度
| In vitro | DMSO | 87 mg/mL (159.47 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
*<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 | 18.33 mL | 91.66 mL | 183.32 mL |
| 0.5 mM | 3.67 mL | 18.33 mL | 36.66 mL |
| 1 mM | 1.83 mL | 9.17 mL | 18.33 mL |
| 5 mM | 0.37 mL | 1.83 mL | 3.67 mL |
*The above data is based on the productmolecular weight 545.5. 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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