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AChE/Aβ-IN-2

Cat. No. M42159
AChE/Aβ-IN-2 Structure
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Quality Control & Documentation
Biological Activity

AChE/Aβ-IN-2 is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor with IC50 of 5.054 μM.

Chemical Information
Molecular Weight 356.89
Formula C20H25ClN4
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] David Gibbs et al. Neurol Clin. Back Pain: Differential Diagnosis and Management

[2] Sowmya Ananthan et al. J Neural Transm (Vienna). Chronic orofacial pain

[3] Paul Glare et al. Lancet. Transition from acute to chronic pain after surgery

[4] Clifford J Woolf. J Clin Invest. What is this thing called pain?

[5] J D Loeser et al. Lancet. Pain: an overview

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