SLF1081851
目录号 : GC66459SLF1081851 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
Sample solution is provided at 25 µL, 10mM.
SLF1081851 is a Spns2 inhibitor, inhibits S1P release (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 IC50 value 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). |
Cas No. | 2763730-97-6 | SDF | Download SDF |
分子式 | C21H33N3O | 分子量 | 343.51 |
溶解度 | 储存条件 | 4°C, protect from light | |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 2.9111 mL | 14.5556 mL | 29.1112 mL |
5 mM | 0.5822 mL | 2.9111 mL | 5.8222 mL |
10 mM | 0.2911 mL | 1.4556 mL | 2.9111 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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