生物活性
GW788388是有效的，口服活性的，选择性的转化生长因子β受体I（TGF-βR1）（激活素受体样激酶5，ALK5）抑制剂,无细胞试验中IC50为18 nM，也抑制TGF-βII型受体和activin II型受体活性，但不抑制BMP II型受体。
靶点信息
| ALK5 (Cell-free assay) | | | | |
| 18 nM | | | | |
化学数据
| 目录号 | A11083 |
| 作用机制 | Inhibitor (抑制剂) |
| M. Wt | 425.5 |
| Formula | C25H23N5O2 |
| 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. | 452342-67-5 |
| Synonyms | GW-788388 |
| SMILES | C1COCCC1NC(=O)C2=CC=C(C=C2)C3=NC=CC(=C3)C4=C(NN=C4)C5=CC=CC=N5 |
溶解度
| In vitro (25°C) | DMSO | 15 mg/mL (35.25 mM) |
| Water | Insoluble |
| Ethanol | Insoluble |
| 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 | 23.5 mL | 117.51 mL | 235.02 mL |
| 0.5 mM | 4.7 mL | 23.5 mL | 47 mL |
| 1 mM | 2.35 mL | 11.75 mL | 23.5 mL |
| 5 mM | 0.47 mL | 2.35 mL | 4.7 mL |
*The above data is based on the productmolecular weight 425.5 . 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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