您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > SLF1081851 TFA
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
SLF1081851 TFA
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SLF1081851 TFA图片
CAS NO:2763730-98-7
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
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].

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).
分子量

457.53

Formula

C23H34F3N3O3

CAS 号

2763730-98-7

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.