羟基波生坦 (Ro 48-5033) 是波生坦 (BOS) 的主要代谢物,由肝脏中的细胞色素 P450 系统代谢。
Cas No. | 253688-60-7 |
别名 | 波生坦羟甲基杂质,Ro 48-5033 |
Canonical SMILES | COC1=CC=CC=C1OC2=C(NS(C3=CC=C(C(C)(CO)C)C=C3)(=O)=O)N=C(C4=NC=CC=N4)N=C2OCCO |
分子式 | C27H29N5O7S |
分子量 | 567.6 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Hydroxy bosentan is an active phase I metabolite of bosentan produced by the cytochrome P450 isoforms CYP3A4 and CYP2C9. Bosentan is an antagonist of the endothelin receptors type A (Ki = 6.5 nM) and type B (Ki = 340 nM). Up to 20% of the activity of bosentan may be due to the action of hydroxy bosentan because even though it has a lower affinity for endothelin receptors, its concentration is 3-fold higher in plasma. |