MPO-IN-1 is a potent, orally active, and irreversible indole-containing inhibitor of myeloperoxidase ( MPO ). MPO-IN-1 has IC 50 s 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.

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 V ss (L/kg) T 1/2 (h) AUC inf (nM?h) p.o. C max (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.

2471981-21-0

C24H21ClN4

400.9

MPO-IN-1

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years