| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: = 100%
| Targets |
Spns2 (Sphingosine-1-phosphate transporter 2); SLF-1081851 is a selective inhibitor of Spns2. Spns2 is a transporter that mediates the export of sphingosine-1-phosphate (S1P) from cells. By inhibiting Spns2, the compound blocks S1P release, thereby reducing extracellular S1P levels. S1P is a key signaling molecule that regulates various physiological processes, including lymphocyte trafficking, angiogenesis, and inflammation. Inhibition of S1P release has therapeutic potential in immune and inflammatory diseases.
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| ln Vitro |
Spns2 keeps lymphatic sphingosine-1-phosphate (S1P), a pleiotropic signaling protein, under check [1]. Compound 16d, SLF1081851 (0-5 μM; 18-20 hours) inhibits S1P release in HeLa cells. SLF1081851 (0-30 μM; 20 minutes) inhibits mSphK1 (recombinant mouse SphK) (10 μM) and mSphK2 (5 μM). The effects of SLF1081851 are dose-dependent, with an IC50 value of 1.93 μM indicating a minimum of 15 times. (IC50 for PhK1 ≥30 μM; IC50 for PhK2 ≈30 μM)[1].
In vitro, SLF-1081851 inhibits S1P release in HeLa cells with an IC₅₀ of 1.93 μM. The compound is used to study the role of Spns2 and S1P in cellular signaling and function. It recapitulates the genetic phenotype of Spns2 null mice, confirming its on-target activity. The compound is typically dissolved in DMSO for in vitro assays. Its effects on S1P release can be measured using mass spectrometry or ELISA-based methods. |
| ln Vivo |
The Spns2 solution's genetic phenotype is repaired and reflux and solution S1P are greatly inhibited by SLF1081851, (20 mg/kg; i.p., post-solution 4) [1].
In vivo, SLF-1081851 is used to study the role of Spns2 and S1P in development and the immune system. By inhibiting S1P release, the compound can modulate immune cell trafficking and inflammatory responses. It recapitulates the genetic phenotype of Spns2 null mice, providing a pharmacological tool to study Spns2 function. The compound may have therapeutic potential in immune-mediated diseases. However, detailed in vivo efficacy and pharmacokinetic data are not extensively documented. |
| Enzyme Assay |
In vitro, HeLa cells are treated with SLF-1081851 at various concentrations, and S1P release into the culture medium is measured. The compound is typically dissolved in DMSO and diluted in cell culture medium. After incubation for a specified time, the medium is collected, and S1P levels are quantified using mass spectrometry or an ELISA-based assay. The IC₅₀ for inhibition of S1P release is determined by plotting the percentage inhibition against the compound concentration. The compound is for research use only.
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| Animal Protocol |
Animal/Disease Models: C57BL/6 mice[1]: 20 mg/kg
Route of Administration: intraperitoneal (ip) injection; blood draw results 4 hrs (hrs (hours)) after taking the drug: circulating lymphocyte count and plasma S1P concentration were Dramatically diminished. Animal/Disease Models: SpragueDawley mice (4 weeks old) [1] Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; single dose; measurement results at 0, 0.5, 1, 2, 4, 6 and 24 hrs (hrs (hours)) after Route of Administration: The maximum concentration of 5 μM is reached in the blood after 2 hrs (hrs (hours)), and the drug level is maintained at ≥ 2 μM for at least 24 hrs (hrs (hours)), proving that the lifespan of rats with half concentration exceeds 8 hrs (hrs (hours)). The appearance of SPNS2-IN-1 in the circulation was associated with a maximal reduction in lymphocyte counts at 4 h (25% reduction compared to time = 0). In vivo, SLF-1081851 is administered to animal models to study the effects of Spns2 inhibition on development and the immune system. The compound is typically administered via intraperitoneal or oral routes. The animals are monitored for changes in immune cell populations, inflammatory responses, and other physiological parameters. The compound recapitulates the genetic phenotype of Spns2 null mice. All procedures are conducted in accordance with institutional animal care guidelines. |
| ADME/Pharmacokinetics |
SLF-1081851 has a molecular weight of 343.51 and the chemical formula C₂₁H₃₃N₃O. It is soluble in DMSO. The compound is supplied as a solid and should be stored at -20°C. It is stable under recommended storage conditions. The compound is for research use only and not for human therapeutic use. Further studies are needed to fully characterize its ADME properties.
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| Toxicity/Toxicokinetics |
Specific toxicity data for SLF-1081851 are not extensively documented. As a Spns2 inhibitor, it may affect immune cell trafficking and inflammatory responses. The compound is for research use only and not for human therapeutic use. It should be handled with appropriate safety precautions, including the use of personal protective equipment. The compound should be stored in a sealed container in a cool, dry place away from incompatible materials.
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| References | |
| Additional Infomation |
SLF-1081851 is also known as SLF1081851. It is a Spns2 inhibitor that inhibits S1P release with an IC₅₀ of 1.93 μM. S1P plays a key role in development and the immune system. The compound recapitulates the genetic phenotype of Spns2 null mice. It is used as a research tool to study Spns2 function and S1P signaling. It is supplied as a solid and should be stored at -20°C. It is for research use only.
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| Molecular Formula |
C21H33N3O
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| Molecular Weight |
343.506225347519
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| Exact Mass |
343.262
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| CAS # |
2763730-97-6
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| Related CAS # |
SLF1081851 TFA;2763730-98-7
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| PubChem CID |
164517202
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| Appearance |
White to off-white solid powder
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| LogP |
6.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
13
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| Heavy Atom Count |
25
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| Complexity |
318
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1C(CCCN)=NC(C2=CC=C(CCCCCCCCCC)C=C2)=N1
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| InChi Key |
VLTITRMWGPJCFJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H33N3O/c1-2-3-4-5-6-7-8-9-11-18-13-15-19(16-14-18)21-23-20(25-24-21)12-10-17-22/h13-16H,2-12,17,22H2,1H3
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| Chemical Name |
3-[3-(4-decylphenyl)-1,2,4-oxadiazol-5-yl]propan-1-amine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
Ethanol : ~10 mg/mL (~29.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.91 mM) (saturation unknown) in 10% EtOH + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 + to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 6.67 mg/mL (19.42 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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