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Art. -Nr.: HY-149004A

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SLF1081851 TFA

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

SLF1081851 (TFA) is a Spns2 inhibitor, inhibits S1P release (IC₅₀=1.93 μM). SLF1081851 (TFA) plays a key role in development and immune system.

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CAS. Nr.: 2763730-98-7
Formel: C₂₃H₃₄F₃N₃O₃
Molecular Weight:457.53

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Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (269 KB)

SLF1081851 TFA Chemical Structure

CAS. Nr.: 2763730-98-7

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

SLF1081851 (TFA) is a Spns2 inhibitor, inhibits S1P release (IC₅₀=1.93 μM). SLF1081851 (TFA) plays a key role in development and immune system^[1]^[2].

IC₅₀ & Target

Spns2 (spinster homologue 2)^[1]

Alle LPL Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Sphingosine 1-phosphate (S1P) is a pleiotropic signaling molecule, and Spns2 exerts the functions to maintain lymph S1P^[1].
SLF1081851 (TFA) (compound 16d) (0-5 μM; 18-20 h) inhibits S1P release with an IC₅₀ value of 1.93 μM in Hela cells^[1].
SLF1081851 (TFA) (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

SLF1081851 (TFA) (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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).

Chemical Information

CAS. Nr. 2763730-98-7
Molecular Weight 457.53
Formel C₂₃H₃₄F₃N₃O₃
SMILES

NCCCC1=NC(C2=CC=C(CCCCCCCCCC)C=C2)=NO1.O=C(O)C(F)(F)F
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (4)

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Cell

Structural and functional insights into Spns2-mediated transport of sphingosine-1-phosphate. [Abstract]

2023 Jun 8;186(12):2644-2655.e16. PMID: 37224812
Cell Commun Signal

Spinster homolog 2/S1P signaling ameliorates macrophage inflammatory response to bacterial infections by balancing PGE2 production. [Abstract]

2024 Sep 30;22(1):463. PMID: 39350143
Int Immunopharmacol

Liquiritigenin attenuates alcohol-induced liver inflammation by regulating the SphK1/S1P/SPNS2 signaling pathway. [Abstract]

2026 Jan 1;168(Pt 2):115881. PMID: 41297343
Pflugers Arch

Sphingosine kinase 1 inhibition aggravates vascular smooth muscle cell calcification. [Abstract]

2025 Jun;477(6):815-826. PMID: 39899071

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Fritzemeier R, et al. Discovery of In Vivo Active Sphingosine-1-phosphate Transporter (Spns2) Inhibitors. J Med Chem. 2022 Jun 9;65(11):7656-7681. [Content Brief]

[2]. Lynch Kevin R, et al. Preparation of oxadiazoles as inhibitors of spinster homolog 2 (SPNS2) for use in therapy: World Intellectual Property Organization, WO2022056042[P]. 2022-03-17.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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SLF1081851 TFA

4 Cited Publications

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (4)
Reinheit & Dokumentation
Verweise

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SLF1081851 TFA

Publications Citing Use of MedChemExpress (MCE) SLF1081851 TFA

Alle LPL Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

SLF1081851 TFA Related Classifications

HY-149004A Related Classifications