生物活性
Macitentan是一种口服活性非肽双重ETA/ETB(内皮素) receptor双重拮抗剂，IC50为0.5 nM/391 nM。用于治疗特发性肺纤维化(IPF)和肺动脉高压(PAH)。
靶点信息
化学数据
| 目录号 | A11492 |
| 作用机制 | Antagonist (拮抗剂) |
| M. Wt | 588.27 |
| Formula | C19H20Br2N6O4S |
| 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. | 441798-33-0 |
| Synonyms | ACT 064992, ACT-064992, ACT064992 |
| SMILES | CCCNS(=O)(=O)NC1=C(C(=NC=N1)OCCOC2=NC=C(C=N2)Br)C3=CC=C(C=C3)Br |
溶解度
| In vitro | DMSO | 87 mg/mL (147.88 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 | 17 mL | 84.99 mL | 169.99 mL |
| 0.5 mM | 3.4 mL | 17 mL | 34 mL |
| 1 mM | 1.7 mL | 8.5 mL | 17 mL |
| 5 mM | 0.34 mL | 1.7 mL | 3.4 mL |
*The above data is based on the productmolecular weight 588.27. 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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