| Bioactivity | 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]. | ||||||||||||
| Target | 2.6 μM (in plasma MPO assay); 0.12 μM (in fluorescent MPO peroxidation assay) | ||||||||||||
| 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 | ||||||||||||
| Name | MPO-IN-1 | ||||||||||||
| CAS | 2471981-21-0 | ||||||||||||
| Formula | C24H21ClN4 | ||||||||||||
| Molar Mass | 400.90 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |