S1P5 receptor antagonist 1 

S1P5 receptor antagonist 1 is a selective, blood-brain barrier-permeable S1P5 receptor antagonist with an EC₅₀ of 0.1 nM and a K_i of 4.4 nM. S1P5 receptor antagonist 1 inhibits the migration of natural killer cells towards sphingosine 1-phosphate in vitro, with no effect on T cell migration. S1P5 receptor antagonist 1 can be used in the research of central nervous system diseases^[1].

The S1P5 receptor antagonist 1 (Compound 15) (1-25000 nM; 1 h pretreatment) inhibits mouse spleen NK cell migration toward S1P with an IC₅₀ of 553 nM, has no effect on mouse spleen naive T cell migration, and shows a biphasic response with increased migration at 100 nM and inhibition at higher doses^[1].
The S1P5 receptor antagonist 1 has favorable in vitro hepatocyte stability, with a Qh% of 30% in rat hepatocytes and 49% in human hepatocytes^[1].

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

S1P5 receptor antagonist 1 (Compound 15) (1-5 mg/kg; p.o., i.v.; single dose) administered to rats results in favorable systemic exposure, 92% oral bioavailability, and consistent brain penetration^[1].

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

437.62

C₂₈H₃₉NO₃

1621065-22-2

C(C=1C2=C(C(C)=CC1O[C@@H]3CC[C@@H](C(C)(C)C)CC3)C=CC=C2)N4CCC(C(O)=O)CC4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Ma B, et al. Novel Potent Selective Orally Active S1P5 Receptor Antagonists. ACS Med Chem Lett. 2021;12(3):351-355. Published 2021 Jan 15.  [Content Brief]