TH5487 is a selective 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC50 of 342 nM. TH5487 (5 μM; 1 hour) decreases TNFα- and LPS-induced proinflammatory gene expression to near pretreatment levels. TH5487 stops OGG1 from recognizing its DNA substrate, inhibits DNA repair and modifies OGG1 chromatin dynamics, which results in the inhibition of proinflammatory pathway genes.
In vivo, TH5487 (prophylactic intraperitoneally injection; 8-30 mg/kg; 1-9 hours) decreases TNFα or LPS induced the robust recruitment of neutrophils to the airways, and reduces the pulmonary neutrophil count in a time-dependent manner.
| Molecular Weight | 541.18 |
| Formula | C19H18BrIN4O2 |
| CAS Number | 2304947-71-3 |
| Solubility (25°C) | DMSO ≥ 13 mg/mL |
| 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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