DprE1-IN-6
DprE1-IN-6 (Compound 56) is a DprE1 inhibitor. DprE1-IN-6 has anti-TB activity against Mtb H37Rv strain (MIC: 1 μM). DprE1-IN-6 also has antimycobacterial activity against drug-resistant strains. DprE1-IN-6 has high microsomal stability and medium clearance.
For research use only. We do not sell to patients.
- CAS No.: 3052383-83-9
- Formula: C22H24N6O
- Molecular Weight:388.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| H9c2 | IC50 |
>50 μM
Compound: 56
|
Cytotoxicity against rat H9c2 cells assessed as cell viability incubated for 72 hrs by MTT spectrophotometric analysis
Cytotoxicity against rat H9c2 cells assessed as cell viability incubated for 72 hrs by MTT spectrophotometric analysis
|
[PMID: 37421887] |
| HepG2 | IC50 |
>50 μM
Compound: 56
|
Cytotoxicity against human HepG2 cells assessed as cell viability incubated for 72 hrs by MTT spectrophotometric analysis
Cytotoxicity against human HepG2 cells assessed as cell viability incubated for 72 hrs by MTT spectrophotometric analysis
|
[PMID: 37421887] |
| HepG2 | IC50 |
63.9 μM
Compound: 56
|
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells incubated for 24 hrs by MTT assay
|
[PMID: 37421887] |
Chemical Information
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CAS No. 3052383-83-9
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Molecular Weight 388.47
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Formula C22H24N6O
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SMILES
CCNC1=C2N(CC3=CC=C4C=CC=CC4=C3)C=NC2=NC(N5CCOCC5)=N1
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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.
Protocols
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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
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)