1204329-34-9
Chemical Structure
BI-9627
- CAS No.: 1204329-34-9
- Formula:C16H19F3N4O2
- Molecular Weight:356.34
IUPAC Name: 4-(1-acetylpiperidin-4-yl)-N-carbamimidoyl-3-(trifluoromethyl)benzamide
InChIKey: QMHRLXNEGYTSRV-UHFFFAOYSA-N
SMILES: NC(NC(C1=CC=C(C2CCN(C(C)=O)CC2)C(C(F)(F)F)=C1)=O)=N
Biological Activity: BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca2+ recovery time in KO hiPSC-CMs. BI-9627 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[1][2][3][4].
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BI-9627 | 99.71% | BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca2+ recovery time in KO hiPSC-CMs. BI-9627 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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- [1]. Huber JD, et al. Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitableprofile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat. J Med Chem. 2012 Aug 23;55(16):7114-40. [Content Brief]
- [2]. Chen, M., et al., (2023). An abnormal LPA/LPAR1-NHE1 axis leads to the autophagy deficiency of trophoblast cells in recurrent spontaneous abortion. Reproduction (Cambridge, England), 166(5), 357–368. [Content Brief]
- [3]. Liang, M., et al., (2024). Flagellar pH homeostasis mediated by Na+/H+ exchangers regulates human sperm functions through coupling with CatSper and KSper activation. Human reproduction (Oxford, England), 39(4), 674–688. [Content Brief]
- [4]. Li, S., et al., (2024). Mitochondrial transplantation rescues Ca2+ homeostasis imbalance and myocardial hypertrophy in SLC25A3-related hypertrophic cardiomyopathy. Cell reports, 43(12), 115065. [Content Brief]
Keywords
