Nodinitib-1 (ML130) is a potent and selective inhibitor of NOD1 with IC50 of 0.56 μM, inhibits NF-κB activation, exhibits 36-fold selectivity over NOD2. Nodinitib-1 selectively inhibits IL-8 production induced by NOD1 ligand. Nodinitib-1 also inhibits γ-tri-DAP-induced expression of the prototypical NF-κB target gene IκBα at the mRNA level. Nodinitib-1 inhibits γ-tri-DAP-dependent activation of NF-κB (IκBα phosphorylation and degradation) and MAPK (p38 phosphorylation) signalings, without affecting Akt survival pathway.
| Molecular Weight | 287.34 |
| Formula | C14H13N3O2S |
| CAS Number | 799264-47-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 20 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.
[5] Gavin Magnuson, et al. High Throughput Screening Assays for NOD1 Inhibitors - Probe 1
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