SLF1081851 |
| رقم الكتالوجGC66459 |
SLF1081851 هو مثبط Spns2 ، يمنع إطلاق S1P (IC50 = 1.93 μ ؛ M). يلعب SLF1081851 دورًا رئيسيًا في تطوير الجهاز المناعي.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2763730-97-6
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Formula | C21H33N3O | M.Wt | 343.51 |
| الذوبان | Storage | 4°C, protect from light | |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
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- Purity: >98.00%
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