The hydroxamate-based AspR1 probe, which shares structural features with GM6001 and TAPI-0 covalently labeled the recombinant chlamydial PDF, and furthermore, GM6001 and TAPI-0 competed off the probe in the labeling of the parasitic enzyme.
| Cell Experiment | |
|---|---|
| Cell lines | pLysS cells |
| Preparation method | Extracts prepared from untransformed pLysS cells or from the bacteria transformed with the pET21-PDF vector were mixed with 1 μM probe in the presence or absence of excessive GM6001 or TAPI-0 or GMNC. |
| Concentrations | 1 μM |
| Incubation time | 1 h |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 456.54 |
| Formula | C24H32N4O5 |
| CAS Number | 143457-40-3 |
| 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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