1897379-34-8

SLM 6031434 Hydrochloride is a Sphk2 inhibitor (Ki = 0.4 μM for mouse Sphk2). Exhibts some selectivity for Sphk2 over Sphk1 (Ki > 20 μM). Decreases levels of sphingosine-1-phosphate (S1P) in U937 cells in vitro and increases blood levels of S1P in wild-type mice.

SLM6031434 is a selective sphingosine (Sph) kinase 2 (SK2SphK2SpK2) inhibitor (r/m SphK2 Ki = 400/500 nMr/m SphK1 Ki >20 μM) th at effectively downregulates cellular sphingosine 1-phosphate (S1P) level (47% S1P & 143% Sph of control in U937 post 2h 100 nM SLM6031434 treatment) and selectively reduces plasma S1P in Sphk1-/-but not Sphk2-/- mice in vivo (5 mg/kg i.v.). In contrary to Sphk2-KO miceSLM6031434 treatment enhances plasma S1P in wild-type mice and offers neuroprotective efficacy against ischemic stroke (2 mg/kg i.v. 2h prior to tMCAO).

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