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S1R agonist 2

Cat. No. M42700
S1R agonist 2 Structure
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Biological Activity

S1R agonist 2 is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively.

Chemical Information
Molecular Weight 309.45
Formula C21H27NO
CAS Number 150085-21-5
Form Liquid
Storage -20°C, sealed
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] Naif A Arishi et al. Cureus. An Overview of Fluvoxamine and its Use in SARS-CoV-2 Treatment

[2] Pasquale Linciano et al. Eur J Med Chem. Novel S1R agonists counteracting NMDA excitotoxicity and oxidative stress: A step forward in the discovery of neuroprotective agents

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

[4] Sándor Váczi et al. Platelets. S1R agonist modulates rat platelet eicosanoid synthesis and aggregation

[5] Timur A Mavlyutov et al. Adv Exp Med Biol. The Sigma-1 Receptor-A Therapeutic Target for the Treatment of ALS?

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