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  3. SLF1081851 TFA

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。

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SLF1081851 TFA Chemical Structure

SLF1081851 TFA Chemical Structure

CAS No. : 2763730-98-7

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SLF1081851 (TFA) is a Spns2 inhibitor, inhibits S1P release (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 IC50 value 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].

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

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].

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

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).
分子量

457.53

Formula

C23H34F3N3O3

CAS 号
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.

纯度 & 产品资料
参考文献

SLF1081851 TFA 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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SLF1081851 TFA
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HY-149004A
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