[(2R)-1-[[4-[[3-(ベンジルスルホニルメチル)-5-メチルフェノキシ]メチル]フェニル]メチル]ピロリジン-2-イル]メタノール

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Warning

• 危険有害性情報

  H302：飲み込むと有害

  H315：皮膚刺激

  H319：強い眼刺激

  H335：呼吸器への刺激のおそれ

• 注意書き

  P261：粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

[(2R)-1-[[4-[[3-(ベンジルスルホニルメチル)-5-メチルフェノキシ]メチル]フェニル]メチル]ピロリジン-2-イル]メタノール 価格

[(2R)-1-[[4-[[3-(ベンジルスルホニルメチル)-5-メチルフェノキシ]メチル]フェニル]メチル]ピロリジン-2-イル]メタノール 化学特性,用途語,生産方法

• 一般的な説明

  A cell-permeable hydroxymethylpyrrolidine compound that acts as a high affinity (K_d = 5 nM, k_offt_1/2 = 8.5 min), but poor, sphingosine kinase-1/SphK1 substrate (1/1,500 of sphingosine processivity) and potently inhibits against SphK1-catalyzed sphingosine-to-S1P conversion (IC₅₀ = 2.0 nM; [sphingosine] = 3 μM) in a reversible, sphingosine-, but not ATP-, competitive manner (K_i = 3.6 nM), exhibiting 132-fold selectivity over SphK2, no affinity toward S1P receptors (S1P1, S1P2, S1P3, S1P5), and much reduced or no inhibitory activity against a panel of 46 other lipid and protein kinases (IC₅₀ >10 μM), including the structurally related diacylglyerol kinase α/DAGKα (3.7% inhibition at 10 μM). PF-543 exposure in 1483 squamous cultures is reported to result in intracellular S1P depletion (by 90% upon 1 h 200 nM or 7 d 1 μM drug exposure) with concomitant elevation of sphingosine level and no detectable cytotoxicity (1 μM for 7 to 9 d in 1483, A549, Jurkat, LN229, MCF7, or U937 cultures). Also active in human whole blood assays in the presence human & bovine serum proteins (IC₅₀ = 26.7 nM against cellular C₁₇-S1P formation from exogenously added 20 μM C₁₇-sphingosine in 10 min with 30 min drug preincubation).

• Biochem/physiol Actions

  PF-543 hydrochloride is a novel, cell-permeable, potent and selective inhibitor of sphingosine kinase-1 (SphK1). PF-543 inhibits SphK1 with a Ki of 3.6 nM, is sphingosine competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 decreased the level of endogenous S1P by 10-fold with proportional increase of the level of sphingosine.

[(2R)-1-[[4-[[3-(ベンジルスルホニルメチル)-5-メチルフェノキシ]メチル]フェニル]メチル]ピロリジン-2-イル]メタノール 生産企業

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[(2R)-1-[[4-[[3-(ベンジルスルホニルメチル)-5-メチルフェノキシ]メチル]フェニル]メチル]ピロリジン-2-イル]メタノール スペクトルデータ(¹HNMR)

1415562-82-1, [(2R)-1-[[4-[[3-(ベンジルスルホニルメチル)-5-メチルフェノキシ]メチル]フェニル]メチル]ピロリジン-2-イル]メタノール キーワード