2471981-21-0

2471981-21-0 structure
2471981-21-0 structure
  • Name: MPO-IN-1
  • Chemical Name: MPO-IN-1
  • CAS Number: 2471981-21-0
  • Molecular Formula: C24H21ClN4
  • Molecular Weight: 400.90
  • Catalog: Research Areas Inflammation/Immunology
  • Create Date: 2022-03-03 12:15:27
  • Modify Date: 2025-08-26 15:34:12
  • 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].

Name MPO-IN-1
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].
Related Catalog
Target

2.6 μM (in plasma MPO assay); 0.12 μM (in fluorescent MPO peroxidation assay)[1]

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.
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.

Molecular Formula C24H21ClN4
Molecular Weight 400.90
Hazard Codes Xi
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