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编 号:F741790
分子式:C21H33N3O
分子量:343.51
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1mg
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5mg
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10mg
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25mg
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50mg
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生物活性:
SLF1081851 is a Spns2 inhibitor, inhibits S1P release (IC50=1.93 μM). SLF1081851 plays a key role in development and immune system.

体内研究:
SLF1081851 (20 mg/kg;ip,给药后 4 小时) 显著抑制循环淋巴细胞和血浆 S1P,并重现 Spns2 缺失小鼠的遗传表型。Animal Model:C57BL/6 mice
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)
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).

体外研究:
Sphingosine 1-phosphate (S1P) 是一种多效性信号分子,Spns2 发挥维持淋巴 S1P 的功能。 SLF1081851 (compound 16d) (0-5 μM;18- 20 小时) 在 Hela 细胞中抑制 S1P 释放,IC50 值为 1.93 μM。 SLF1081851 (0-30 μM;20 分钟) 抑制 mSphK1 (重组小鼠 SphK) (10 μM) 和 mSphK2 (5 μM) 呈剂量依赖性,表明选择性至少为 15 倍 (SphK1 IC50≥30 μM;SphK2 IC 50≈30 μM)。
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