NGP 555 has very good brain penetration/absorption, distribution, metabolism, and excretion (ADME) properties. It efficiently crosses the blood-brain barrier, has a brain:plasma ratio of 0.93 (in Tg2576 mice) and shows in vivo efficacy for lowering the biomarker Aβ42 in rodent studies for brain and plasma. Chronic administration of NGP 555 (milled into chow) to Tg2576 mice results in a significant reduction of amyloid plaques.
| Cell Experiment | |
|---|---|
| Cell lines | SH-SY5Y-APP cells |
| Preparation method | SH-SY5Y-APP cells are treated with various concentrations of NGP 555 or NGP 328, in triplicate wells, for 18 hours. Media is collected and analyzed for Aβ peptides using Meso Scale triplex ELISA (Aβ38, Aβ40, and Aβ42) and total Aβ ELISA. |
| Concentrations | 10 nM-100 μM |
| Incubation time | 18 h |
| Animal Experiment | |
|---|---|
| Animal models | Sprague-Dawley male rats |
| Formulation | 80% PEG |
| Dosages | 0-37.5 mg/kg |
| Administration | oral administration |
| Molecular Weight | 406.52 |
| Formula | C23H23FN4S |
| CAS Number | 1304630-27-0 |
| Form | Solid |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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