YYA-021 is a CD4-mimic HIV entry inhibitor, competitively inhibiting the interaction between gp120 and CD4.
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Rats and rhesus macaques |
| Formulation | Converted to its hydrochloride salt by treatment with 4 M HCl in dioxane. |
| Dosages | 14 mg/kg (rats), 13.4 mg/kg (rhesus macaques) |
| Administration | i.v |
| Molecular Weight | 317.43 |
| Formula | C18H27N3O2 |
| CAS Number | 144217-65-2 |
| Form | Solid |
| Solubility (25°C) | 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.
[1] Takaaki Mizuguchi, et al. A minimally cytotoxic CD4 mimic as an HIV entry inhibitor
[2] Chie Hashimoto, et al. A CD4 mimic as an HIV entry inhibitor: pharmacokinetics
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