NPD-2975
Based on 1 Customer Validation
NPD-2975 (compound 30) is an orally active antitrypanosomal agent, against Human African Trypanosomiasis (HAT). NPD-2975 has low toxicity potential against human MRC-5 lung fibroblasts, and acute mouse model of T. b. brucei infection. NPD-2975 shows acceptable metabolic stability, inhibits T. b. brucei with IC500 of 70 nM in vitro. NPD-2975 also inhibits CYP enzymes resulted in IC50 values of 0.16 and 0.42 μM against CYP1A2 and CYP2C19, respectively.
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- Pureté : 98.40%
- CAS No.: 3032452-65-3
- Formule: C14H13FN4O
- Masse moléculaire:272.28
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
Description
IC50 & Target
IC50: 70 nM (Trypanosoma brucei), 0.16 μM (CYP1A2), 0.42 μM (CYP2C19)[1]
In Vivo
Pharmacokinetic Analysis of NPD-2975 in Mouse Model[1]
| Route | Dose (mg/kg) | Tmax (h) | Cmax (μM) | T1/2 (h) | AUC0-6 h (ng·h/mL) | Cl (mL/min) |
| PO | 50 | 1 | 5.25 | 3.46 | 6064.75 | 58.5 |
| IP | 10 | 13.18 | 1.06 | 3928.37 | 171 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3032452-65-3
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Appearance Solid
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Masse moléculaire 272.28
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Formule C14H13FN4O
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Color White to off-white
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SMILES
O=C1C(NN=C2C(C)C)=C2N=C(C3=CC=C(F)C=C3)N1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Protocole
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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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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How to Choose the Right Model Animal
Choosing the right model animal is a validity-driven decision in which the species, strain, sex, age, genetic background, disease-induction method, outcome measures, and welfare burden must match the scientific question rather than laboratory tradition or convenience. A model should be selected by judging face validity, construct validity, and predictive validity: whether it resembles the human phenotype, whether it reproduces relevant mechanisms, and whether results are likely to predict human biology or treatment response. Animal studies often fail to translate because of species differences, weak disease resemblance, poor experimental design, inadequate reporting, publication bias, and underuse of randomization, blinding, and sample-size justification. Unresolved questions include how to rank competing models objectively, how much human-disease complexity must be reproduced for a given objective, and when non-animal systems such as organoids, ex vivo tissue, or computational models
Pureté et documentation
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Fiche technique (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)