SLF1081851 是一种 Spns2 抑制剂，抑制 S1P 释放 (IC50=1.93 μM)。SLF1081851 在发育和免疫系统中起关键作用。
| Cas No. | 2763730-97-6 |
| 分子式 | C21H33N3O |
| 分子量 | 343.51 |
| 储存条件 | 4°C, protect from light |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | SLF1081851 is aSpns2inhibitor, inhibitsS1Prelease (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 IC50value 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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