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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.
| Molecular Weight | 392.8 |
| Formula | C16H20ClF3N4O2 |
| CAS Number | 1422252-46-7 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL (ultrasonic) Water 4.17 mg/mL (ultrasonic and warming and heat to 60°C) |
| Storage | 4°C, dry, sealed |
[1] Chuangchuang Xu, et al. Org Biomol Chem. Metal-free and regiospecific synthesis of 3-arylindoles
[3] No authors listed. Carteolol
[5] S Groszkowski, et al. Pol J Pharmacol Pharm. 1-Haloacylpiperazines
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| FR183998 free base
FR183998 free base is a potent Na+/H+-exchange inhibitor, with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pHi change in rat lymphocytes, rat and human platelets, respectively. |
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