A dual SPHK1 and SPHK2 inhibitor (Kis = 0.73 and 0.9 µM

SLC5111312 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
1870811-01-0
Storage:
-20
UN-No:
Non-Hazardous - /

SLC5111312 is a dual inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2 (Kis = 0.73 and 0.9 µM, respectively, using human recombinant kinases).{38412} SLC5111312 binding is selective for Sphk2 over Sphk1 in mice (Kis = 1 and 20 µM, respectively) but not rat (Kis = 1.1 and 0.8 µM, respectively).{38413} It decreases cell-associated sphingosine-1-phosphate (S1P) and increases sphingosine in U937 monocytic leukemia cells at concentrations of 0.1 and 0.3 µM. SLC5111312 (10 mg/kg) also decreases S1P in vivo in Sphk1-/- but not in Sphk2-/- mice and in rat, showing a functional selectivity for Sphk2 in mice.  

 

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SKU: 23288 - 1 mg Category:

Description

A dual SPHK1 and SPHK2 inhibitor (Kis = 0.73 and 0.9 µM, respectively, using human recombinant kinases); selective for Sphk2 over Sphk1 in mice (Kis = 1 and 20 µM, respectively); not selective in rat (Kis = 1.1 and 0.8 µM for Sphk2 and Sphk1, respectively); decreases S1P in vitro at concentrations of 0.1 and 0.3 µM; decreases S1P in Sphk1-/- knockout mice and in rat at a dose of 10 mg/kg

Formal name: (2S,3S)-3-hydroxy-2-[3-[6-(pentyloxy)-2-naphthalenyl]-1,2,4-oxadiazol-5-yl]-1-pyrrolidinecarboximidamide, monohydrochloride

Synonyms: 

Molecular weight: 445.9

CAS: 1870811-01-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Lipid Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Lipid Biochemistry|Sphingolipids

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