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S1PR1 Radioligand 1

Cat. No. M41859
S1PR1 Radioligand 1 Structure
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Biological Activity

S1PR1 Radioligand 1is a specific S1PR1 radioligand with IC50 = 8.7 nM.

Chemical Information
Molecular Weight 471.42
Formula C22H22F5N3O3
CAS Number 2845249-11-6
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] Hao Jiang et al. ACS Chem Neurosci. Quantitative Analysis of S1PR1 Expression in the Postmortem Multiple Sclerosis Central Nervous System

[2] Ganesh B Chand et al. Front Psychiatry. Differential Sphingosine-1-Phosphate Receptor-1 Protein Expression in the Dorsolateral Prefrontal Cortex Between Schizophrenia Type 1 and Type 2

[3] Hao Jiang et al. ACS Chem Neurosci. InVitro and In Vivo Investigation of S1PR1 Expression in the Central Nervous System Using [3H]CS1P1 and [11C]CS1P1

[4] Hui Liu et al. Mol Imaging Biol. In vivo Characterization of Four 18F-Labeled S1PR1 Tracers for Neuroinflammation

[5] Hui Liu et al. Mol Imaging Biol. Upregulated Sphingosine 1-Phosphate Receptor 1 Expression in Human and Murine Atherosclerotic Plaques

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