SLP7111228
SLP7111228 is a selective sphingosine kinase 1 (SphK1) inhibitor and anti-inflammatory agent. SLP7111228 selectively inhibits SphK1 and reduces the production of sphingosine-1-phosphate. SLP7111228 decreases lipopolysaccharide-induced TNFα and IL-1β levels. SLP7111228 alleviates obliterative pulmonary arteriopathy, increases cardiac index and decreases total pulmonary vascular resistance index. SLP7111228 can be used in research related to neuroinflammatory diseases and pulmonary hypertension.
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- CAS No.: 1449765-82-5
- Formule: C22H33N5O
- Masse moléculaire:383.53
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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SphK1 |
IL-1β |
TNF-α |
SLP7111228 (1 µM; 30 min pre-incubation, 4 h LPS incubation) significantly reduces LPS-induced IL-1β mRNA expression in BV2 mouse microglia cells, with a non-significant reduction in TNFα mRNA expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BV2 mouse microglia cells
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Concentration:1 µM
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Incubation Time:30 min (pre-incubation); 4 h (incubation with LPS)
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Result:Significantly reduced LPS-induced IL-1β mRNA expression.
Reduced TNFα mRNA expression, but this effect was not statistically significant due to high variability between experiments.
Showed the same level of inhibition of LPS-induced TNFα and IL-1β mRNA expression as either inhibitor used alone when combined with the SphK2 inhibitor SLM6031434 (HY-120268).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (adult male, ~250 g, Su/Hx/Nx model)[2]
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Dosage:10 mg/kg
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Administration:i.p.; daily; 3 weeks
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Result:Significantly decreased plasma S1P levels without affecting sphingosine levels.
Reduced vascular occlusion in small, medium, and large pulmonary arteries.
Reduced diastolic right ventricular internal diameter (RVID) in correlation with lower S1P.
Improved cardiac index and decreased total pulmonary artery resistance index.
Does not alter right ventricular pressure, hypertrophy, systemic pressure, or heart rate.
Chemical Information
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CAS No. 1449765-82-5
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Masse moléculaire 383.53
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Formule C22H33N5O
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SMILES
CCCCCCCCC(C=C1)=CC=C1C2=NOC(C[C@H]3N(CCC3)C(N)=N)=N2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Standoli S, et al. Sphingosine Kinases at the Intersection of Pro-Inflammatory LPS and Anti-Inflammatory Endocannabinoid Signaling in BV2 Mouse Microglia Cells. Int J Mol Sci. 2023 May 9;24(10):8508. [Content Brief]
[2]. Gairhe S, et al. Sphingosine-1-phosphate is involved in the occlusive arteriopathy of pulmonary arterial hypertension. Pulm Circ. 2016;6(3):369-380. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)