NS-181
NS-181 is an orally active MetAP2 inhibitor and antiamebic agent with oral effectiveness.NS-181 functionally inhibits methionine aminopeptidase 2, a protein critical for Entamoeba histolytica proliferation. NS-181 exerts antiamebic activity against Entamoeba histolytica, leading to resolution of amebic liver abscess. NS-181 can be used for the research of amebiasis.
For research use only. We do not sell to patients.
- CAS No.: 3075693-63-6
- Formula: C24H28O7
- Molecular Weight:428.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
NS-181 (30 min) resists hamster liver microsome-mediated metabolism and retains potent antiamebic activity (ED50 of 14.6 nM) after 30 min of microsomal incubation[1].
NS-181 (10 μM) exhibits no cytotoxicity against Huh-7 human hepatocellular carcinoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:unstated specific strain[1]
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Dosage:15 mg/kg (subcutaneous); 30 mg/kg (oral)
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Administration:s.c.; 5 consecutive days; p.o.; 5 consecutive days
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Result:Achieved complete resolution of amebic liver abscess, with abscess weight proportion relative to whole liver reduced to near 0%, amebic mRNA levels in liver reduced, and inflammation levels decreased to match noninfected controls.
Significantly reduced amebic liver abscess size, with abscess weight proportion relative to whole liver markedly decreased compared to vehicle controls.
Chemical Information
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CAS No. 3075693-63-6
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Molecular Weight 428.47
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Formula C24H28O7
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SMILES
O=C(O[C@H](C(CC1)=O)[C@@]([C@@]2(C)O[C@@H]2C/C=C(C)\C)(O)[C@]31CO3)/C=C/C4=CC=CC(O)=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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