D-赤式鞘氨醇作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetD-erythro-SphingosineCat. No.: HY-101047CAS No.: 123-78-4分式: CHNO分量: 299.49作靶點(diǎn): PKC; Phosphatase; Endogenous Metabolite作通路: Epigenetics; TGF-beta/Smad; Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 41.67 mg/mL (139.14 mM; Need

2、 ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲(chǔ)備液1 mM 3.3390 mL 16.6950 mL 33.3901 mL5 mM 0.6678 mL 3.3390 mL 6.6780 mL10 mM 0.3339 mL 1.6695 mL 3.3390 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)

3、您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天 使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (6.95 mM); Clear solution此案可獲得 2.08 mg/mL (6.95 mM

4、，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (6.95 mM); Clear solution此案可獲得 2.08 mg/mL (6.95 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 20.8 mg/mL 的

5、澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。Page 1 of 2 www.MedChemEBIOLOGICAL ACTIVITY物活性 D-erythro-Sphingosine (Erythrosphingosine) 種常有效的 p32 激酶活化劑，EC50 為 8 M。D-erythro- Sphingosine 抑制蛋激酶 C (PKC)。D-erythro-Sphingosine (Erythrosphingosine) 也 種 PP2A 激活劑。IC & Target p32 PKC PP2A Human Endogenous8 M (EC50) Metabolite體

6、外研究 A p32-sphingosine-activated protein kinase responds to low concentrations of D-erythro-Sphingosine with an initialactivation observed at 2.5 M and a peak activity at 10-20 M. This kinase shows a modest specificity for D-erythro-Sphingosine over other sphingosine tereoisomers, and a preference fo

7、r sphingosines over ihydrosphingosines1. D-erythro-Sphingosine inhibits protein kinase C in vitro2. D-erythro-Sphingosine has been shown to inhibit proteinkinase C, which affects cell regulation and several signal transduction pathways, and exhibits antitumor promoteractivities in various mammalian

8、cells3.REFERENCES1. Pushkareva MYu, et al. Regulation of sphingosine-activated protein kinases: selectivity of activation by sphingoid basesand inhibition by non-esterifiedfatty acids. Biochem J. 1993 Sep 15;294 ( Pt 3):699-703.2. Khan WA, et al. Protein kinase C and platelet inhibition by D-erythro

9、-Sphingosine: comparison with N,N-dimethylsphingosine and commercialpreparation. Biochem Biophys Res Commun. 1990 Oct 30;172(2):683-91.3. Pham VT, et al. A concise synthesis of a promising protein kinase C inhibitor: D-erythro-Sphingosine. Arch Pharm Res. 2007 Jan;30(1):22-7.4. Cheng P, et al. Protein phosphatase 2A (PP2A) activation promotes axonal growth and recovery in the CNS. J Neurol Sci. 2015 Dec 15;359(1-2):48-56.McePdfHeightCaution: Product has not been fully validated for medical application