SLF80821178
Based on 1 publication(s) in Google Scholar
SLF80821178 is an orally active Spns2 inhibitor that inhibits S1P release with an IC50 of 51 nM in HeLa cells. SLF80821178 blocks Spns2-mediated S1P transport/release, induces lymphopenia, and reduces circulating B cell, NK cell, and T cell populations. SLF80821178 can be used for research on multiple sclerosis.
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- Pureté : 99.70%
- CAS No.: 2764877-61-2
- Formule: C21H35N3O
- Masse moléculaire:345.52
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) SLF80821178
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Activité biologique
Description
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Spns2 |
S1P |
In Vitro
SLF80821178 blocks S1P release in adult dermal LECs, with a pIC50 of 7.64[2].
SLF80821178 (10 µM) only moderately inhibits recombinant SphK1 and SphK2 at a concentration of 10 µM[3].
SLF80821178 inhibits S1P release from cultured human dermal LECs with an IC50 of 23 nM[3].
SLF80821178 inhibits S1P release from HeLa cells expressing mouse Spns2, with an IC50 of 53 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Chronic SLF80821178 (20 mg/kg/day; i.p.; daily; for 14 days; additional dose on Day 15) decreases ALCs without changing plasma S1P and with minimal effect on lymph S1P in mice[2].
Chronic SLF80821178 (20 mg/kg/d; i.p.; once daily; 15 days) produces lymphopenia without changing plasma S1P and only minimally affects lymph S1P[3].
Acute SLF80821178 (20 mg/kg; i.p.; single dose) reduces blood lymphocytes without significantly changing lymph S1P[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6j[1]
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Dosage:3, 10, 30 mg/kg (intraperitoneal); 10, 100 mg/kg (oral gavage)
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Administration:intraperitoneal injection; oral gavage
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Result:Intraperitoneal administration of SLF80821178 at 3, 10, and 30 mg/kg decreased circulating lymphocyte counts, reaching a maximum level of 50%.
Oral gavage administration produced dose-dependent lymphocytopenia, with the 100 mg/kg dose achieving maximum effect.
After oral administration of 10 mg/kg, lymphocyte counts measured at 4 h showed a maximum level of lymphopenia (~50%).
No change in plasma S1P levels was observed when SLF80821178 was administered intraperitoneally or orally.
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Animal Model:C57BL/6J (female, 10 weeks old)[2]
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Dosage:10 mg/kg; 30 mg/kg
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Administration:p.o.; once daily; starting Day 10 for 14 days
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Result:Produced a dose-dependent decrease in peak disease score (Days 15-19) and a decrease in chronic disease score (Days 25-28) compared with vehicle control mice.
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Animal Model:C57BL/6J (male and female cohorts)[2]
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Dosage:20 mg/kg/day
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Administration:i.p.; daily; for 14 days; additional dose on Day 15
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Result:Chronic SLF80821178 administration decreased ALCs, with a maximal decrease of 50% (compared with approximately 90% for SRMs).
Plasma S1P concentrations were unchanged.
Lymph S1P concentrations were minimally affected.
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Animal Model:C57BL/6J (female, 10 weeks old)[3]
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Dosage:30 mg/kg/d
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Administration:p.o.; once daily; for 14 days beginning day 10 after immunization
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Result:Decreased the peak disease score during days 15-19 and decreased chronic disease scores during days 25-28 compared with vehicle control mice.
Efficacy was similar to that reported in inducible Spns2-deficient mice.
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Animal Model:C57BL/6J (both sexes, 6-8 weeks old)[3]
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Dosage:20 mg/kg/d
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Administration:i.p.; once daily; for 15 days
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Result:Chronic SLF80821178 evoked lymphopenia on day 15, measured as reduced peripheral blood lymphocyte counts.
Plasma S1P concentrations were not affected.
Lymph S1P concentrations showed minimal effect.
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Animal Model:C57BL/6[3]
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Dosage:20 mg/kg
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Administration:i.p.; single dose
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Result:Substantially decreased circulating lymphocyte counts.
No significant effect on lymph S1P concentration was observed.
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Animal Model:C57BL/6J[3]
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Dosage:20 mg/kg
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Administration:i.p.; single dose
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Result:Reduced circulating B cells, NK cells, and T cells.
Its effect on T lymphocytes, particularly CD4+ cells, was proportionally less than that of Fingolimod (HY-11063).
Chemical Information
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CAS No. 2764877-61-2
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Appearance Solid
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Masse moléculaire 345.52
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Formule C21H35N3O
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Color White to off-white
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SMILES
O=C(N1CCNCC1)NC2=CC=C(CCCCCCCCCC)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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PLoS Pathog
A Spinster-like Transporter at the Inner Membrane Complex is critical for Toxoplasma gondii cytokinesis, motility and invasion. [Abstract]2026 Jan 28;22(1):e1013886. PMID: 41604433
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (289.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.8942 mL | 14.4709 mL | 28.9419 mL | 72.3547 mL |
| 5 mM | 0.5788 mL | 2.8942 mL | 5.7884 mL | 14.4709 mL | |
| 10 mM | 0.2894 mL | 1.4471 mL | 2.8942 mL | 7.2355 mL | |
| 15 mM | 0.1929 mL | 0.9647 mL | 1.9295 mL | 4.8236 mL | |
| 20 mM | 0.1447 mL | 0.7235 mL | 1.4471 mL | 3.6177 mL | |
| 25 mM | 0.1158 mL | 0.5788 mL | 1.1577 mL | 2.8942 mL | |
| 30 mM | 0.0965 mL | 0.4824 mL | 0.9647 mL | 2.4118 mL | |
| 40 mM | 0.0724 mL | 0.3618 mL | 0.7235 mL | 1.8089 mL | |
| 50 mM | 0.0579 mL | 0.2894 mL | 0.5788 mL | 1.4471 mL | |
| 60 mM | 0.0482 mL | 0.2412 mL | 0.4824 mL | 1.2059 mL | |
| 80 mM | 0.0362 mL | 0.1809 mL | 0.3618 mL | 0.9044 mL | |
| 100 mM | 0.0289 mL | 0.1447 mL | 0.2894 mL | 0.7235 mL |
SLF80821178 Related Classifications
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