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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1449765-82-5
- 分子式: C22H33N5O
- 分子量:383.53
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[2]|
SphK1 |
IL-1β |
TNF-α |
体外実験
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).
体内実験
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.
化学情報
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CAS 番号 1449765-82-5
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分子量 383.53
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)