SLF1081851 TFA_product_DataBase

Bioactivity	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].
Target	Spns2 (spinster homologue 2)
Invitro	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].
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]. Animal Model:
Name	SLF1081851 TFA
CAS	2763730-98-7
Formula	C23H34F3N3O3
Molar Mass	457.53
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.

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