Antitrypanosomal agent 6
Antitrypanosomal agent 6 (compound 18a) is a potent and antitrypanosomal agent with favorable ADME properties. Antitrypanosomal agent 6 is > 2-fold more potent against Trypanosoma brucei (T. brucei) than Nifurtimox, with an IC50 value of 0.47 μM. Antitrypanosomal agent 6 has strong interaction to DNA and can bind with high selectivity to AT-rich DNA.
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- CAS 番号: 2492436-35-6
- 分子式: C22H29Cl2N5O
- 分子量:450.40
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
製品説明
IC50 & Target
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Trypanosoma |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| L6 | IC50 |
>250 μM
Compound: 18a
|
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
|
[PMID: 32927230] |
化学情報
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CAS 番号 2492436-35-6
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分子量 450.40
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分子式 C22H29Cl2N5O
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SMILES
CCN(CCOC1=CC=C(C2=NC3=CC(C4=NCCN4)=CC=C3N2)C=C1)CC.[H]Cl.[H]Cl
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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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
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)