SLF1081851 (TFA) 是一种Spns2抑制剂，抑制S1P释放 (IC50=1.93 μM)。SLF1081851 (TFA) 在发育和免疫系统中起关键作用。
| 生物活性 | SLF1081851 (TFA) is aSpns2inhibitor, inhibitsS1Prelease (IC50=1.93 μM). SLF1081851 (TFA) plays a key role in development and immune system[1][2]. |
| IC50& Target | Spns2 (spinster homologue 2)[1] |
体外研究
(In Vitro) | Sphingosine 1-phosphate (S1P) is a pleiotropic signaling molecule, and Spns2 exerts the functions to maintain lymph S1P[1].
SLF1081851 (TFA) (compound 16d) (0-5 μM; 18-20 h) inhibits S1P release with an IC50value of 1.93 μM in Hela cells[1].
SLF1081851 (TFA) (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].
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体内研究
(In Vivo) | SLF1081851 (TFA) (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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
