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NS 1738

Cat. No. M30193
NS 1738 Structure
Synonym:

NSC 213859

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Biological Activity

NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).

Chemical Information
Molecular Weight 365.13
Formula C14H9Cl2F3N2O2
CAS Number 501684-93-1
Form Solid
Solubility (25°C) DMSO ≥ 100 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] Spencer R Pierce, et al. Biomolecules. Mutational Analysis of Anesthetic Binding Sites and Their Effects on GABAA Receptor Activation and Modulation by Positive Allosteric Modulators of the α7 Nicotinic Receptor

[2] Zsolt Kristóf Bali, et al. Sci Rep. Facilitation and inhibition of firing activity and N-methyl-D-aspartate-evoked responses of CA1 hippocampal pyramidal cells by alpha7 nicotinic acetylcholine receptor selective compounds in vivo

[3] Kateryna Uspenska, et al. Int J Biochem Cell Biol. Positive allosteric modulators of α7* or β2* nicotinic acetylcholine receptors trigger different kinase pathways in mitochondria

[4] Katarzyna M Targowska-Duda, et al. J Biomol Struct Dyn. Molecular interactions of type I and type II positive allosteric modulators with the human α7 nicotinic acetylcholine receptor: an in silico study

[5] Guanglin Kuang, et al. Phys Chem Chem Phys. Theoretical study of the binding profile of an allosteric modulator NS-1738 with a chimera structure of the α7 nicotinic acetylcholine receptor

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Keywords: NS 1738, NSC 213859 supplier, AChR/AChE, inhibitors, activators

 
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