SLF80821178 hydrochloride
Based on 1 publication(s) in Google Scholar
SLF80821178 hydrochloride is an orally active Spns2 inhibitor that inhibits S1P release with an IC50 of 51 nM in HeLa cells. SLF80821178 hydrochloride blocks Spns2-mediated S1P transport/release, induces lymphopenia, and reduces circulating B cell, NK cell, and T cell populations. SLF80821178 hydrochloride can be used for research on multiple sclerosis.
For research use only. We do not sell to patients.
- CAS No.: 2764877-62-3
- Formula: C21H36ClN3O
- Molecular Weight:381.98
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Publications Citing Use of MedChemExpress (MCE) SLF80821178 hydrochloride
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Biological Activity
Description
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Spns2 |
S1P |
In Vitro
SLF80821178 hydrochloride blocks S1P release in adult dermal LECs, with a pIC50 of 7.64[2].
SLF80821178 hydrochloride (10 µM) only moderately inhibits recombinant SphK1 and SphK2 at a concentration of 10 µM[3].
SLF80821178 hydrochloride inhibits S1P release from cultured human dermal LECs with an IC50 of 23 nM[3].
SLF80821178 hydrochloride 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 hydrochloride (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 hydrochloride (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 hydrochloride (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. 2764877-62-3
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Molecular Weight 381.98
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Formula C21H36ClN3O
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SMILES
O=C(N1CCNCC1)NC2=CC=C(CCCCCCCCCC)C=C2.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SLF80821178 hydrochloride Related Classifications
HY-162655A Related Classifications
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