生物活性
Asenapine maleate平对多种受体具有高亲和力（pKi），包括5-羟色胺5-HT1A（8.6），5-HT1B（8.4），5-HT2A（10.2），5-HT2B（9.8），5-HT2C（10.5），5 -HT5A（8.8），5-HT6（9.5）和5-HT7（9.9）受体，肾上腺素α1（8.9），α2A（8.9），α2B（9.5）和α2C（8.9）受体，多巴胺D1（ 8.9），D2（8.9），D3（9.4）和D4（9.0）受体以及组胺H1（9.0）和H2（8.2）受体。
Targets
| Target | Value |
| 5-HT2C | pki: 10.46 |
| 5-HT2A | pki: 10.15 |
| 5-HT7 | pki: 9.94 |
| 5-HT2B | pki: 9.75 |
| 5-HT6 | pki: 9.6 |
| α2B-adrenergicreceptor | pki: 9.49 |
| D3receptor | pki: 9.38 |
| H1receptor | pki: 9 |
| D4receptor | pki: 8.95 |
| α1A-adrenergicreceptor | pki: 8.93 |
| α2C-adrenergicreceptor | pki: 8.91 |
| D2LReceptor | pki: 8.9 |
| α2A-adrenergicreceptor | pki: 8.9 |
| D1receptor | pki: 8.85 |
| 5-HT5A | pki: 8.84 |
| D2SReceptor | pki: 8.84 |
| 5-HT1A | pki: 8.6 |
| 5-HT1B | pki: 8.4 |
| H2receptor | pki: 8.21 |
化学数据
| 目录号 | A10091 |
| 作用机制 | Antagonist (拮抗剂) |
| M. Wt | 401.84 |
| Formula | C17H16ClNO.C4H4O4 |
| 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. | 85650-56-2 |
| SMILES | CN1C[C@H]2[C@H](C1)C3=C(C=CC(=C3)Cl)OC4=CC=CC=C24.C(=C\C(=O)O)\C(=O)O |
溶解度
| In vitro | DMSO | 78 mg/mL (194.1 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 | 24.89 mL | 124.43 mL | 248.86 mL |
| 0.5 mM | 4.98 mL | 24.89 mL | 49.77 mL |
| 1 mM | 2.49 mL | 12.44 mL | 24.89 mL |
| 5 mM | 0.5 mL | 2.49 mL | 4.98 mL |
*The above data is based on the productmolecular weight 401.84. 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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