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NPD-2975
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Catalog No. T79568
NPD-2975 (compound 30) is an orally active antitrypanosomal agent effective against Human African Trypanosomiasis (HAT), demonstrating acceptable metabolic stability and low toxicity potential in human MRC-5 lung fibroblasts, as well as in an acute mouse model of T. b. brucei infection. It exhibits an in vitro IC50 of 70 nM against T. b. brucei and IC50 values of 0.16 μM and 0.42 μM against CYP1A2 and CYP2C19 enzymes, respectively [1].
NPD-2975
NPD-2975
😃Good
Catalog No. T79568
NPD-2975 (compound 30) is an orally active antitrypanosomal agent effective against Human African Trypanosomiasis (HAT), demonstrating acceptable metabolic stability and low toxicity potential in human MRC-5 lung fibroblasts, as well as in an acute mouse model of T. b. brucei infection. It exhibits an in vitro IC50 of 70 nM against T. b. brucei and IC50 values of 0.16 μM and 0.42 μM against CYP1A2 and CYP2C19 enzymes, respectively [1].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $143 | 35 days | |
| 5 mg | $668 | 35 days | |
| 10 mg | $1,260 | 35 days |
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Product Introduction
Bioactivity
Chemical Properties
| Description | NPD-2975 (compound 30) is an orally active antitrypanosomal agent effective against Human African Trypanosomiasis (HAT), demonstrating acceptable metabolic stability and low toxicity potential in human MRC-5 lung fibroblasts, as well as in an acute mouse model of T. b. brucei infection. It exhibits an in vitro IC50 of 70 nM against T. b. brucei and IC50 values of 0.16 μM and 0.42 μM against CYP1A2 and CYP2C19 enzymes, respectively [1]. |
| In vivo | NPD-2975 administered orally (25 mg/kg, twice daily for five consecutive days; gavage) enhanced survival rates during the initial phase in a murine model of HAT infection [1]. Pharmacokinetic analysis of NPD-2975 in mice [1] revealed the following parameters for the oral (PO) and intraperitoneal (IP) routes: PO—Dose: 50 mg/kg, T_max: 1 h, C_max: 5.25 μM, T_1/2: 3.46 h, AUC_0-6 h: 6064.75 ng·h/mL, Cl: 58.5 mL/min; IP—Dose: 10 mg/kg, T_max: 13.18 h, C_max: 1.06 μM, T_1/2: 3928.37 h, AUC_0-6 h: 171 ng·h/mL. |
| Molecular Weight | 272.28 |
| Formula | C14H13FN4O |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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