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Necrostatin 2 racemate

Cat. No. M10602
Necrostatin 2 racemate Structure
Synonym:

Nec-1s; Necrostatin 1S; 7-Cl-O-Nec-1

Size Price Availability Quantity
2mg USD 88  USD88 In stock
5mg USD 135  USD135 In stock
10mg USD 235  USD235 In stock
25mg USD 435  USD435 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
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.
Chemical Information
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
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Peter Mikus, et al. Molecules. Determination of Novel Highly Effective Necrostatin Nec-1s in Rat Plasma by High Performance Liquid Chromatography Hyphenated with Quadrupole-Time-of-Flight Mass Spectrometry

[2] N Takahashi, et al. Cell Death Dis. Necrostatin-1 analogues: critical issues on the specificity, activity and in vivo use in experimental disease models

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Keywords: Necrostatin 2 racemate, Nec-1s; Necrostatin 1S; 7-Cl-O-Nec-1 supplier, RIPK, inhibitors, activators


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