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Synonyms:
DNDI-VL-2098
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | DNDI-VL-2098 is an orally active antileishmanial agent known for its high permeability and in vitro metabolic stability. It selectively inhibits CYP2C19 with an IC50 of 0.47 μM and does not affect other major CYP enzymes (CYP1A2, CYP2C9, CYP2D6, and CYP3A4) at concentrations up to 12.5 μM. The compound exhibits favorable pharmacokinetic properties across various animal models including mice, hamsters, rats, and dogs. DNDI-VL-2098 is characterized by moderate to high plasma protein binding, making it suitable for visceral leishmaniasis research. |
| Targets & IC50 | CYP2C19:0.47 μM |
| In vitro | DNDI-VL-2098 (0.3-30 μg/mL; 4 h) exhibits moderate to high plasma protein binding rates (94-98%) with a free fraction of 3-6% in samples from mice, rats, dogs, and humans. It shows potent activity in an amastigote macrophage model with an IC50 of 0.025 μM against antimony-resistant Leishmania donovani DD8 strains and an IC50 of 0.7-2.6 μM against African clinical isolates. |
| In vivo | DNDI-VL-2098, when administered at a dose of 50 mg/kg orally once daily for five consecutive days, achieved over 99% parasite inhibition in an acute visceral leishmaniasis mouse model. In a chronic visceral leishmaniasis hamster model, DNDI-VL-2098 at 25 mg/kg demonstrated more than 85% parasite inhibition, showing superior efficacy compared to its racemic mixture and (S)-enantiomer. |
| Molecular Weight | 359.26 |
| Formula | C14H12F3N3O5 |
| Cas No. | 681492-17-1 |
| Smiles | C(OC1=CC=C(OC(F)(F)F)C=C1)[C@]2(C)OC=3N(C2)C=C(N(=O)=O)N3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
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