生物活性
ONX 0914是有效，选择性的免疫蛋白酶体亚基LMP7的抑制剂，在自身免疫性疾病（如类风湿性关节炎，炎性肠病和狼疮）中具有潜在的治疗应用。ONX 0914被设计为一种有效的免疫蛋白酶抑制剂，对组成型蛋白酶体的交叉反应最小。
靶点信息
| LMP7 (Cell-free assay) | | | | |
| ~10 nM | | | | |
化学数据
| 目录号 | A12653 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 580.67 |
| Formula | C31H40N4O7 |
| 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. | 960374-59-8 |
| Synonyms | ONX0914, ONX 0914, PR-957 |
| SMILES | C[C@@H](C(=O)N[C@@H](CC1=CC=C(C=C1)OC)C(=O)N[C@@H](CC2=CC=CC=C2)C(=O)[C@]3(CO3)C)NC(=O)CN4CCOCC4 |
溶解度
| In vitro (25°C) | DMSO | 87 mg/mL (149.82 mM) |
| Water | Insoluble |
| Ethanol | 87 mg/mL (149.82 mM) |
| In vivo | 2% DMSO+castor oil | 9 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 | 17.22 mL | 86.11 mL | 172.21 mL |
| 0.5 mM | 3.44 mL | 17.22 mL | 34.44 mL |
| 1 mM | 1.72 mL | 8.61 mL | 17.22 mL |
| 5 mM | 0.34 mL | 1.72 mL | 3.44 mL |
*The above data is based on the productmolecular weight 580.67. 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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