S1PR5-IN-1 

S1PR5-IN-1 (Compound 7a) is a highly selective S1PR5 antagonist and orally bioavailable inhibitor with a human S1PR5 IC₅₀ of 85.4 nM and human S1PR5 K_d of 2.173 nM.S1PR5-IN-1 binds to S1PR5 and inhibits natural killer cell migration toward sphingosine-1-phosphate.S1PR5-IN-1 can be used for the research of multiple sclerosis^[1].

[¹⁸F]S1PR5-IN-1 (Compound 7a) (0.02-33 nM) binds specifically and with high affinity to recombinant human S1PR5 cell membranes, with a K_d of 2.173 nM^[1].
[¹⁸F]S1PR5-IN-1 (6.25-800 nM; 45 min) binds specifically to S1PR5 in C57BL/6 mouse brain tissue, with a K_d of 4.6 nM and a Bmax of 427.2 fmol/mg^[1].
[¹⁸F]S1PR5-IN-1 (6.25-800 nM; 45 min) binds specifically to S1PR5 in post-mortem human cerebral cortex tissue, with a K_d of 27.6 nM and a B_max of 381.6 fmol/mg^[1].
[¹⁸F]S1PR5-IN-1 (~370 kBq per slide; 1 h) shows significantly reduced binding in brain sections from cuprizone-fed C57BL/6J mice compared to controls, reflecting decreased S1PR5 expression associated with demyelination^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

[¹⁸F]S1PR5-IN-1 (Compound 7a) (~1.48 MBq; i.v.; single injection) demonstrates sustained, high brain uptake in healthy male Sprague-Dawley rats over a 120-minute period, with no significant in vivo defluorination^[1].
[¹⁸F]S1PR5-IN-1 (~15-22 MBq; i.v.; single injection) exhibits specific in vivo binding to S1PR5 in healthy male C57BL/6 mouse brains, as demonstrated by altered uptake following pretreatment with S1PR5 modulators (4 mg/kg; i.v.; 5 min pre-injection)^[1].
[¹⁸F]S1PR5-IN-1 (~15-22 MBq; i.v.; single injection) detects reduced S1PR5 expression associated with cuprizone-induced demyelination in female C57BL/6J mice, with a 22.0% reduction in whole-brain SUV compared to control mice^[1].
[¹⁸F]S1PR5-IN-1 (~158 MBq; i.v.; single injection) demonstrates rapid, high brain uptake and sustained retention in healthy male rhesus macaques, with regional uptake matching known primate S1PR5 expression patterns^[1].
[¹⁸F]S1PR5-IN-1 (~44.4 MBq (rat), ~0.13 GBq (macaque); i.v.; single injection) exhibits high metabolic stability in healthy rats and rhesus macaques, with no brain-penetrant radiometabolites detected in either species^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

441.58

C₂₇H₃₆FNO₃

3107268-28-7

Solid

White to off-white

CC(C)([C@@H]1CC[C@@H](OC2=CC(F)=C3C(C=CC=C3)=C2CN4CCC(CC4)C(O)=O)CC1)C

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [1]. Lang J, et al. Design and Synthesis of Novel PET Radiotracers for Imaging Sphingosine-1-Phosphate Receptor 5 (S1PR5) in the Brain. J Med Chem. 2025;68(12):12991-13018.  [Content Brief]