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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- CAS. Nr.: 2922402-01-3
- Formel: C23H25N3O
- Molecular Weight:359.46
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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.
| 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 % |
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.
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Animal Model:C57BL/6j (male, 8 weeks old) treated thioglycolate broth[1]
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Dosage:30, 150 mg/kg
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Administration:i.g.; single dose
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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.
Chemical Information
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CAS. Nr. 2922402-01-3
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Molecular Weight 359.46
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Formel C23H25N3O
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SMILES
O=C1N(C2=CC=C(C=CN3)C3=C2)C[C@@H](C4=CC=C([C@H]5CCCN5)C=C4)[C@@H]1C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
MPO-IN-10 Related Classifications
HY-186046 Related Classifications
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