Antitrypanosomal agent 7
Antitrypanosomal agent 7 (compound 18c) is a potent and antitrypanosomal agent with favorable ADME properties. Antitrypanosomal agent 7 is > 2-fold more potent against Trypanosoma brucei (T. brucei) than Nifurtimox, with an IC50 value of 0.71 μM. Antitrypanosomal agent 7 has strong interaction to DNA and can bind with high selectivity to AT-rich DNA.
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- CAS No.: 2492436-38-9
- Formule: C23H31Cl2N5O2
- Masse moléculaire:480.43
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
Description
IC50 & Target
IC50: 0.71 μM (T. brucei)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L6 | IC50 |
>250 μM
Compound: 18c
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Cytotoxicity against rat L6 cells incubated for 6 days by resazurin dye based assay
Cytotoxicity against rat L6 cells incubated for 6 days by resazurin dye based assay
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[PMID: 32927230] |
Chemical Information
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CAS No. 2492436-38-9
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Masse moléculaire 480.43
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Formule C23H31Cl2N5O2
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SMILES
COC1=CC(C2=NC3=CC(C4=NCCN4)=CC=C3N2)=CC=C1OCCN(CC)CC.[H]Cl.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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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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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)