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PRE-084 

Cat. No. M28307
PRE-084  Structure
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Biological Activity

PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.

Chemical Information
Molecular Weight 317.42
Formula C19H27NO3
CAS Number 138847-85-5
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Mohanapriya Kumaran, et al. Mol Biol Rep. PRE-084 ameliorated kidney injury by reducing endoplasmic reticulum stress in the rat model of adenine-induced chronic kidney disease

[2] Christelle Lasbleiz, et al. Redox Biol. Sigma-1 receptor agonist PRE-084 confers protection against TAR DNA-binding protein-43 toxicity through NRF2 signalling

[3] C V Haritha, et al. Tissue Cell. PRE-084 ameliorates adenine-induced renal fibrosis in rats

[4] Zeinab Y Motawe, et al. Int J Biochem Cell Biol. PRE-084 as a tool to uncover potential therapeutic applications for selective sigma-1 receptor activation

[5] Qi-Jun Gao, et al. Chin Med J (Engl). Sigma-1 Receptor Stimulation with PRE-084 Ameliorates Myocardial Ischemia-Reperfusion Injury in Rats

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