烏苯美司作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetBestatinCat. No.: HY-B0134CAS No.: 58970-76-6分式: CHNO分量: 308.37作靶點(diǎn): Aminopeptidase; Bacterial作通路: Metabolic Enzyme/Protease; Anti-infection儲存式: 4C, sealed storage, away from moisture* In solvent : -80C, 6 months; -20C, 1 month (sealed storage, away frommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 8.3

2、3 mg/mL (27.01 mM; Need ultrasonic)SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.2429 mL 16.2143 mL 32.4286 mL5 mM 0.6486 mL 3.2429 mL 6.4857 mL10 mM 0.3243 mL 1.6214 mL 3.2429 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (sealed storage, away

3、 from moisture)。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，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；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 0.83

4、 mg/mL (2.69 mM); Clear solution此案可獲得 0.83 mg/mL (2.69 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 8.3 mg/mL 的澄 DMSO 儲備液加到 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. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 0.83 mg/mL (2.69 mM); Clear solution此案可獲得 0.83 mg/mL (2.

5、69 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 8.3 mg/mL 的澄 DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合Page 1 of 2 www.MedChemE均勻。3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 0.83 mg/mL (2.69 mM); Clear solution此案可獲得 0.83 mg/mL (2.69 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 8.3 mg/mL 的澄 DMSO 儲備液加

6、到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Bestatin種天然，譜，競爭性的氨肽酶抑制劑。體外研究 Bestatin enhances ATRA-induced differentiation and inhibits ATRA-driven phosphorylation of p38 MAPK in ATRA-sensitive APL NB4 cells. Bestatin can not reverse the differentiation block in ATRA-resistant APL MR2 cells. CD13ligation w

7、ith anti-CD13 antibody WM-15 results in phosphorylation of p38 MAPK, reduces the inhibition of Bestatinon the phosphorylation of p38 MAPK, and completely abolishes the enhancement of Bestatin on ATRA-inducingdifferentiation in NB4 cells2. Bestatin (600 M)-treated cells progress slower through the ce

8、ll cycle due to decreasedrate of cell growth and the frequency of cell division. Bestatin inhibits the frequency of mitosis and the inherentmultinuclearity in D. discoideum, and is not cytotoxic to D. discoideum cells at 0-600 M. Bestatin inhibitsaminopeptidase activity in lysates of PsaA-GFP- and G

9、FP-expressing cells by 69.39% 10.5% and 39.93% 18.7% ofcontrol, respectively4.體內(nèi)研究 Bestatin (20 M) significantly reduces CD13 expression in diabetic mice and results a significant inhibition of MMP-9specific gelationolytic band densities compared to diabetic vehicle-treated mice. Bestatin treatment

10、significantlyinhibits the expression of VEGF and heparanase in diabetic mice. Intravitreal bestatin treatment significantlydownregulates the expression of both HIF-1 and VEGF in diabetic mice retinas. Furthermore, the upregulatedexpression of heparanase in diabetic mice retinas is significantly inhi

11、bited by intravitreal bestatin treatment1. Bestatin(10, 1, and 0.1mg/kg, i.p.) treatment before the antigen-potentiated humoral response to SRBC results in an increasednumber of splenocytes producing hemolytic anti-SRBC antibodies (PFC) and the 2-ME-resistant serum hemagglutinintiter (at a dose of 0

12、.1 mg/kg). Bestatin (1 and 0.1 mg/kg) administered to mice five times on alternate days aftercyclophosphamide injection does not change the suppressive effect of the drug regarding the number of PFC, andeven causes the further decrease of the total anti-SRBC hemagglutinins at dose of 1 mg/kg on day

13、7 after antigenstimulation3.PROTOCOLKinase Assay 4 Cells are harvested, washed, and lysed in NP-40 lysis buffer (50 mM Tris-HCl pH 7.5, 150 mM NaCl, 0.5% NP-40).Total cell protein is quantified using the Bradford assay and 1-mg/mL protein aliquots are made. Ten microliters oftotal cell protein is mi

14、xed with 290 L of substrate solution (0.1 mg/mL dithiothreitol DTT, 0.1 mg/mL albumin, and1 mM alanine-naphthylamide). Fluorometric measurements (340 nm excitation, 400 nm emission) are made after15 and 30 min. The slope of the line between the 15- and 30-min measurements is used to represent aminop

15、eptidaseactivity. Total cell protein is preincubated with bestatin, amastatin, puromycin, EDTA, and/or ZnCl2 for 20 min beforethe fluorometric aminopeptidase assay.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 4 Growing cells (1106 to 2106

16、cells/mL) are diluted to 1.0103 cells/mL and transferred (3 mL) into a well in a 12-well multiwell plate (2.5-cm diameter/well). Cells are treated with 0, 10, 50, 100, 300, or 600 M Bestatin and allowedto grow at 21C shaking at 180 rpm for 48 h. A hemocytometer is used to measure cell density after

17、0, 24, and 48 h.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Page 2 of 3 www.MedChemEAnimal Bestatin is dissolved in PBS. The agent (doses of 10, 1, and 0.1 mg/kg) is injected i.p. to non-cyclophosphamide-Administration 3 treated mice, 5 or 10 times

18、at 24-h intervals before SRBC immunization. The mice are immunized 24 h after the lastdose of bestatin. Pharmacological immunosuppression is induced by a single intraperitoneal injection ofcyclophosphamide administered at a dose of 350 mg/kg, 12 days before SRBC immunization. Bestatin at the doses o

19、f1 and 0.1 mg/kg is injected to cyclophosphamide-immunosuppressed mice i.p. five times at 48-h intervals or 10times at 24-h intervals before SRBC immunization. The first dose of bestatin is administered 24 h aftercyclophosphamide, while the last dose of the drug is injected 24h before SRBC immunizat

20、ion.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Med Chem. 2017 Mar 9;60(5):1817-1828. Int J Oncol. 2019 Jul;55(1):331-339.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Hossain A, et al. Protective effects of bestatin in the retina of streptozotocin-induced diabetic mice. Exp Eye Res. 2016 Aug;149:100-62. Qian X, et al. Inhibition of p38 MAPK Phosphorylation Is Critical for Bestatin to Enhance ATRA-Induce