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E1R 

Cat. No. M28136
E1R  Structure
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Biological Activity

E1R is a positive allosteric modulator of sigma-1 receptors (Sig1R PAM) with cognition-enhancing activity.

Chemical Information
Molecular Weight 232.28
Formula C13H16N2O2
CAS Number 1301211-78-8
Form Solid
Solubility (25°C) DMSO 60 mg/mL (ultrasonic)
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] Edijs Vavers, et al. Front Pharmacol. Allosteric Modulators of Sigma-1 Receptor: A Review

[2] Edijs Vavers, et al. Behav Brain Res. The activity of selective sigma-1 receptor ligands in seizure models in vivo

[3] N N Wang, et al. World J Microbiol Biotechnol. Purification and characterization of a potential antifungal protein from Bacillus subtilis E1R-J against Valsa mali

[4] Xiaoning Gao, et al. Biomed Res Int. Endophytic Bacillus subtilis strain E1R-J is a promising biocontrol agent for wheat powdery mildew

[5] L Zvejniece, et al. Br J Pharmacol. The cognition-enhancing activity of E1R, a novel positive allosteric modulator of sigma-1 receptors

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