DDD100097
Based on 1 Customer Validation
DDD100097 is a potent acyltransferase (TbNMT) inhibitor with an IC50 value of 2 nM. DDD100097 can significantly improve blood-brain barrier permeability. DDD100097 can be used in the study of African trypanosomiasis.
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- Pureza : 99.93%
- No. CAS: 1215012-74-0
- Fòrmula: C22H30Cl2F2N4O2S
- Peso molecular:523.47
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MRC5 | EC50 |
0.001 μM
Compound: 40
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Antitrypanosomal activity against Trypanosoma brucei BSF427 expressing VSG118 infected in human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
Antitrypanosomal activity against Trypanosoma brucei BSF427 expressing VSG118 infected in human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
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[PMID: 25412409] |
| MRC5 | EC50 |
1 μM
Compound: 40
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Antiproliferative activity against human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
Antiproliferative activity against human MRC5 cells assessed as reduction cell viability incubated for 69 hrs by rezasurin dye based assay
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[PMID: 25412409] |
| MRC5 | EC50 |
1 μM
Compound: 68
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CYtotoxicity against human MRC5 cells after 69 hrs by resazurin assay
CYtotoxicity against human MRC5 cells after 69 hrs by resazurin assay
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[PMID: 29125744] |
Chemical Information
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No. CAS 1215012-74-0
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Appearance Solid
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Peso molecular 523.47
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Fòrmula C22H30Cl2F2N4O2S
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SMILES
O=S(C1=C(Cl)C=C(CCCC2CCN(C)CC2)C=C1Cl)(N(C(F)F)C3=C(C)N(C)N=C3C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Protocolo
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Pureza y Documentación
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Ficha de datos (268 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Brand S, et al. Lead optimization of a pyrazole sulfonamide series of Trypanosoma brucei N-myristoyltransferase inhibitors: identification and evaluation of CNS penetrant compounds as potential treatments for stage 2 human African trypanosomiasis. J Med Chem. 2014 Dec 11;57(23):9855-69. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)