2. Apoptosis Metabolic Enzyme/Protease
  3. Glutathione Peroxidase
  4. MPO-IN-10

MPO-IN-10 is an orally active, selective, and irreversible inhibitor of myeloperoxidase (MPO), with an IC50 of 0.080 μM against human MPO. MPO-IN-10 exhibits higher selectivity for extracellular MPO over intracellular (neutrophil) MPO. MPO-IN-10 can be used in the study of inflammatory diseases such as vascular disorders.

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MPO-IN-10

MPO-IN-10 Chemical Structure

CAS No. : 2922402-01-3

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MPO-IN-10 Related Antibodies

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Description

MPO-IN-10 is an orally active, selective, and irreversible inhibitor of myeloperoxidase (MPO), with an IC50 of 0.080 μM against human MPO. MPO-IN-10 exhibits higher selectivity for extracellular MPO over intracellular (neutrophil) MPO. MPO-IN-10 can be used in the study of inflammatory diseases such as vascular disorders[1].

In Vitro

MPO-IN-10 (Compound IN-4) inhibits immune complex-stimulated NETosis in human primary neutrophils with an IC50 of 0.147 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

MPO-IN-10 Related Antibodies
Parmacokinetics
Species Dose Route CLplasma Vdss T1/2 AUClast Cmax Tmax Bioavailability
Mice[1] 1 mg/kg i.v. 69 mL/min/kg 10 L/kg 1.1 h 641 nM·h / / /
Mice[1] 10 mg/kg p.o. / / / 338 nM·h 101 nM 1.3 h 54 %
Rat[1] 1 mg/kg i.v. 29 mL/min/kg 8 L/kg 2.5 h 1574 nM·h / / /
Rat[1] 3 mg/kg p.o. / / / 1672 nM·h 183 nM 2.5 h ~100 %
Dog[1] 0.3 mg/kg i.v. 9 mL/min/kg 7.3 L/kg 8.6 h 4000 nM·h / / /
Dog[1] 3 mg/kg p.o. / / / 4893 nM·h 361 nM 2 h ~100 %
In Vivo

MPO-IN-10 (30-150 mg/kg; oral gavage; single dose) exhibits a dose-dependent inhibition of plasma MPO activity in a murine peritonitis model, with the 150 mg/kg dose achieving nearly complete inhibition[1].
MPO-IN-10 (10-100 mg/kg; oral gavage; single dose) exhibits a dose-dependent inhibition of plasma MPO activity in a mouse model of acute Western diet feeding[1].
MPO-IN-10 (approximately 30-250 mg/kg; oral gavage; 10 days) exhibits a dose-dependent inhibition of plasma MPO activity in mice fed a Western-style diet, with an IC50 of approximately 0.5 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6j (male, 8 weeks old) treated thioglycolate broth[1]
Dosage: 30, 150 mg/kg
Administration: i.g.; single dose
Result: Reduced plasma MPO activity by 69% at 30 mg/kg and reduced plasma MPO activity by ~100% at 150 mg/kg at 5 hours post-dose.
Molecular Weight

359.46

Formula

C23H25N3O
CAS No.
SMILES

O=C1N(C2=CC=C(C=CN3)C3=C2)C[C@@H](C4=CC=C([C@H]5CCCN5)C=C4)[C@@H]1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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MPO-IN-10 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MPO-IN-102922402-01-3Glutathione Peroxidaseinflammatory conditionsratsdogsneutrophilsmiceneutrophil extracellular trap formatioInhibitorinhibitorinhibit

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