SLF1081851 |
| Katalog-Nr.GC66459 |
SLF1081851 ist ein Spns2-Inhibitor, hemmt die S1P-Freisetzung (IC50=1,93 μM). SLF1081851 spielt eine SchlÜsselrolle in der Entwicklung und im Immunsystem.
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Cas No.: 2763730-97-6
Sample solution is provided at 25 µL, 10mM.
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SLF1081851 is a Spns2 inhibitor, inhibits S1P release (IC50=1.93 μM). SLF1081851 plays a key role in development and immune system[1][2].
Sphingosine 1-phosphate (S1P) is a pleiotropic signaling molecule, and Spns2 exerts the functions to maintain lymph S1P[1].
SLF1081851 (compound 16d) (0-5 μM; 18-20 h) inhibits S1P release with an IC50 value of 1.93 μM in Hela cells[1].
SLF1081851 (0-30 μM; 20 min) inhibits mSphK1 (recombinant mouse SphK) (10 μM) and mSphK2 (5 μM) in a dose-dependent manner and suggests at least 15-fold selectivity (SphK1 IC50≥30 μM; SphK2 IC50≈30 μM)[1].
SLF1081851 (20 mg/kg; i.p., 4 h postdose) significantly inhibits circulating lymphocytes and plasma S1P, and recapitulates the genetic phenotype of Spns2 null mice[1].
| Animal Model: | C57BL/6 mice[1] |
| Dosage: | 20 mg/kg |
| Administration: | Intraperitoneal injection; blood was drawn 4 h postdose |
| Result: | Significantly decreased circulating lymphocyte count and plasma S1P concentration. |
| Animal Model: | SpragueDawley mice (4-week-old)[1] |
| Dosage: | 10 mg/kg |
| Administration: | Intraperitoneal injection; single dose; measured at 0, 0.5, 1, 2, 4, 6, and 24 h postdose |
| Result: | Reached a maximum concentration of 5 μM in blood at 2 h with drug levels sustained at ≥ 2 μM for at least 24 h, proved a half-life of over 8 h in rats. The appearance of SPNS2-IN-1 in circulation correlated with a maximal decrease in lymphocyte count at 4 h (25% lower compared to time =0). |
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