| Description |
MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase (MPO). MPO-IN-1 has IC50s of 2.6 μM and 5.3 μM for MPO and thyroid peroxidase (TPO), respectively. MPO-IN-1 inhibits MPO activity in an acute mouse model of inflammation[1].
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| Related Catalog |
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| Target |
2.6 μM (in plasma MPO assay); 0.12 μM (in fluorescent MPO peroxidation assay)[1]
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| In Vivo |
MPO-IN-1 (compound 2) (5 and 90 mg/kg; p.o.; four hours post-Zymosan A administration) significantly reduces MPO activity in a mouse peritonitis model of acute inflammation[1]. Mouse pharmacokinetic parameter of MPO-IN-1[1]. Dose Vss (L/kg) T1/2 (h) AUCinf (nM•h) p.o. Cmax (nM) p.o. PPB (%) 1/10 mg/kg i.v./p.o. 9.8 2.6 2486 502 99.6 Animal Model: Male C57BL/6J mice (mouse peritonitis model of acute inflammation)[1] Dosage: 5 and 90 mg/kg Administration: p.o. (four hours post-Zymosan A administration) Result: Resulted in a ~50% reduction in the MPO activity at 90 mg/kg.
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| References |
[1]. Patnaik A, et al. Discovery of a novel indole pharmacophore for the irreversible inhibition of myeloperoxidase (MPO). Bioorg Med Chem. 2020;28(12):115548.
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