LmCPB-IN-2
LmCPB-IN-2 is an orally active covalent antimalarial agent and Leishmania cysteine protease B (CPB) inhibitor with an IC50 of 4.3 μM. LmCPB-IN-2 reduces parasite burden in the liver and spleen.
For research use only. We do not sell to patients.
- CAS No.: 109924-24-5
- Formula: C16H21N3O3
- Molecular Weight:303.36
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Leishmania |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Peritoneal macrophage | CC50 |
>300 μM
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Cytotoxicity against murine peritoneal macrophages assessed as viability reduction after 24 hrs incubation by MTT/PMS assay, with CC50 >300 μM.
Cytotoxicity against murine peritoneal macrophages assessed as viability reduction after 24 hrs incubation by MTT/PMS assay, with CC50 >300 μM.
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42992041 |
| Peritoneal macrophage | EC50 |
4.6 μM
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Inhibition of intracellular L. amazonensis amastigotes in murine peritoneal macrophages assessed as infection index reduction after 24 hrs exposure by Giemsa staining.
Inhibition of intracellular L. amazonensis amastigotes in murine peritoneal macrophages assessed as infection index reduction after 24 hrs exposure by Giemsa staining.
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42992041 |
| Peritoneal macrophage | EC50 |
3.9 μM
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Inhibition of intracellular L. infantum amastigotes in murine peritoneal macrophages assessed as infection index reduction after 24 hrs exposure by Giemsa staining.
Inhibition of intracellular L. infantum amastigotes in murine peritoneal macrophages assessed as infection index reduction after 24 hrs exposure by Giemsa staining.
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42992041 |
In Vitro
LmCPB-IN-2 (0.43-43 μM), as a mixed-type inhibitor of LmCPB2.8ΔCTE, decreases Vmax from 669.4 to 155.5 RFU·min−1 and decreases Km from 14.1 to 2.3 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Murine peritoneal macrophages
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Concentration:2.34-300 μM
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Incubation Time:24 h
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Result:Showed a CC50 of >300 μM.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, 6 weeks old, 27 g)[1]
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Dosage:0.77 mg/kg/day
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Administration:oral gavage; once daily; 5 consecutive days
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Result:Splenic parasite burden was reduced by approximately 55% by LDU index and 47% by limiting dilution.
In the liver, parasite burden was reduced by 44% by LDU index and 41% by limiting dilution.
Chemical Information
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CAS No. 109924-24-5
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Molecular Weight 303.36
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Formula C16H21N3O3
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SMILES
O=C(OC(C)(C)C)N[C@@H](CC1=CC=CC=C1)C(NCC#N)=O
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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)
LmCPB-IN-2 Related Classifications
HY-191437 Related Classifications
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