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  3. 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.

NS-181

NS-181 Chemical Structure

CAS No. : 3075693-63-6

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Description

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[1].

In Vitro

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.

In Vivo

NS-181 (15-30 mg/kg; s.c., p.o.; 5 consecutive days) achieves complete resolution of amebic liver abscess in hamsters at 15 mg/kg subcutaneous administration and significant reduction in abscess size at 30 mg/kg oral administration[1].

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

Animal Model: unstated specific strain[1]
Dosage: 15 mg/kg (subcutaneous); 30 mg/kg (oral)
Administration: s.c.; 5 consecutive days; p.o.; 5 consecutive days
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.
Molecular Weight

428.47

Formula

C24H28O7

CAS No.
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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Room temperature in continental US; may vary elsewhere.

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
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  • 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.

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Product Name:
NS-181
Cat. No.:
HY-181644
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