BI-9627 hydrochloride 是一种钠氢交换异构体 1 (NHE1) 抑制剂，在细胞内 pH 恢复 (pHi) 和人血小板溶胀试验中 IC50 值为 6 和 31 nM。BI-9627 hydrochloride 对 NHE2 的选择性大于 30 倍，对 NHE3 没有明显的抑制活性。BI-9627 hydrochloride 表现出较低的 DDI (活性分子-活性分子相互作用) 潜力，在大鼠和犬体内良好的药代动力学，在离体心脏缺血-再灌注损伤模型中表现出显著的活性。 BI-9627 hydrochloride is potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor, with IC50s of 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury.
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BI-9627 hydrochloride
CAS number：1422252-46-7 molecular formula：C16H19F3N4O2(free)
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| Chinese alias | 4-(1-乙酰基-4-哌啶基)-N-(氨基亚氨基甲基)-3-(三氟甲基)苯甲酰胺盐酸盐 | ||
| English alias | BIX Hydrochloride | BIX HCl | Benzamide, 4-(1-acetyl-4-piperidinyl)-N-(aminoiminomethyl)-3-(trifluoromethyl)-, hydrochloride | ||
| CAS number | 1422252-46-7 | molecular formula | C16H19F3N4O2(free) |
| molecular weight | 356.34(free) g/mol | Exact mass | - |
| PSA | 102.000 Ų | logp | - |
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