SLM6031434 (hydrochloride) 是一种高度选择性的鞘氨醇激酶 2 (SphK2) 抑制剂,对 mSphK2、rSphK2、mSphK1 和 rSphK1 的 Kis 分别为 0.4 μM、0.5 μM、\u003e20 μM、22 μM。
Cas No. | 1897379-34-8 |
Canonical SMILES | N=C(N)N1CCC[C@H]1C2=NC(C3=CC(C(F)(F)F)=C(C=C3)OCCCCCCCC)=NO2.Cl |
分子式 | C22H30F3N5O2• HCl |
分子量 | 490 |
溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 5 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | SLM6031434 is an inhibitor of sphingosine kinase 2 (SPHK2) (Ki = 0.4 μM for the recombinant mouse enzyme).1 It is selective for SPHK2 over SPHK1 (Kis = >20 μM). It decreases sphingosine-1-phosphate and increases sphingosine levels in U937 monocytic leukemia cells in a concentration-dependent manner. SLM6031434 (5 mg/kg) reduces blood S1P levels in Sphk1-/-, but not Sphk2-/-, mice. SLM6031434 also increases blood S1P levels in wild-type mice and rats. |1. Kharel, Y., Morris, E.A., Congdon, M.D., et al. Sphingosine kinase 2 inhibition and blood sphingosine 1-phosphate levels. J. Pharmacol. Exp. Ther. 355(1), 23-31 (2015). |