Necrostatin-2 racemate (also known as 7-Cl-O-Nec-1 and Nec-1s) is a potent and specific receptor-interacting protein kinase 1 (RIPK1) inhibitor lacking the IDO-targeting effect, with >1000-fold more selective for RIPK1 than for any other kinase out of 485 human kinases.
In vivo, Nec-1s is effective in reducing brain injuries. It is a superior inhibitor suitable for use in vivo lacking a paradoxical sensitizing effect in TNF-induced lethality. Nec-1s possesses several advantageous pharmacokinetic and pharmacodynamic characteristics in comparison to Nec-1. Safety profile of Nec-1s is also superior to that of Nec-1 for reduced in vivo and in vitro toxicity.
Cell Experiment | |
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Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
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Animal models | TNF-induced SIRS model (Female C57BL/6J WT mice) |
Formulation | DMSO (6%) dissolved in endotoxin-free PBS |
Dosages | 0.6 mg/kg and 6 mg/kg |
Administration | i.v. |
Molecular Weight | 277.71 |
Formula | C13H12ClN3O2 |
CAS Number | 852391-15-2 |
Solubility (25°C) | DMSO ≥ 50 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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