1、Product Data SheetTigecyclineCat. No.: HY-B0117CAS No.: 220620-09-7分式: CHNO分量: 585.65作靶點: Bacterial; Autophagy作通路: Anti-infection; Autophagy儲存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數據體外實驗 DMSO : 150 mg/mL (256.13 mM; Need ultrasonic)H2O : 50 mg/mL (85.38 mM; Need ultrasonic)Sol

2、ventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.7075 mL 8.5375 mL 17.0750 mL5 mM 0.3415 mL 1.7075 mL 3.4150 mL10 mM 0.1708 mL 0.8538 mL 1.7075 mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內使，-20C 儲存時，請在 1 個內使。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解

3、案。以下溶解案都請先按照 In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結果的可靠性，澄 的儲備液可以根據儲存條件，適當保存；體內實驗的作液，建議您現現配，當天使； 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沉淀、析出現象，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: 2.5 mg/mL (4.27 mM); Clear solution此案可獲得 2.5 mg/mL (4.27 mM，飽和度未知) 的澄清溶液。以 1 mL

4、作液為例，取 100 L 25.0 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: 2.5 mg/mL (4.27 mM); Clear solution此案可獲得 2.5 mg/mL (4.27 mM，飽和度未知) 的澄清溶液。Page 1 of 2 www.MedChemE以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄均勻。

5、DMSO 儲備液加到 900 L 20% 的 SBE-CD 理鹽溶液中，混合BIOLOGICAL ACTIVITY物活性 Tigecycline (GAR-936) 種譜的氨酰環素抗素。Tigecycline 對 E. coli (MG1655菌株) 的平均抑制濃度 (MIC) 約 為 125 ng/ mL1。對 Acinetobacter baumannii (A. baumannii) 的 MIC50 和 MIC90 分別為 1 和 2 mg/L2。IC & Target Mean MIC: 125 ng/mL (E. coli)1MIC50: 1 mg/mL (A. baumannii)

6、2MIC90: 2 mg/mL (A. baumannii)2體外研究 Tigecycline (0.63-30 M, preincubated for 4 days, treated for 72 h) inhibits AML2 cells and HL-60 cells with IC50s of4.720.54 and 3.060.85 M (freshly prepared). Tigecycline inhibits AML2 cells and HL-60 cells with IC50s of5.640.55 and 4.270.45 M (1 day preincubatio

7、n). Tigecycline inhibits AML2 cells and HL-60 cells with IC50s of5.020.60 and 4.390.44 M (2 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC50s of4.090.41 and 3.950.39 M (3 day preincubation). After a 4 day preincubation of Tigecycline in saline, Tigecyclinelost its abilit

8、y to kill TEX human leukemia cells (from IC505 M when freshly prepared to IC5050 M after 4 dayspreincubation) as measured by CellTiter Flour assay1.Cell Viability Assay1Cell Line: Human leukemic OCI-AML2, HL-60 (ATCC) and TEX cell linesConcentration: 0.63-30 MIncubation Time: Preincubated for 4 days

9、, treated for 72 hoursResult: Inhibited AML2 cells and HL-60 cells with IC50s of 4.720.54 and 3.060.85 M(freshly prepared).體內研究Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) reduces tumor volume and weight inNOD/SCID mice1.The peak plasma concentration (Cmax), the termin

10、al half-life (t1/2), area under the plasma concentration-time curve(AUC), clearance (CL) and volume of distribution (Vz) are 22.8g/mL, 108.9 min, 1912.2min*g/mL, 26.1 mL/min/kg,4109.4 mL/kg for Tigecycline in saline, respectively. The peak plasma concentration (Cmax), the terminal half-life (t1/2),a

11、rea under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are15.7g/mL,110.3 min, 2036.5 min*g/mL, 24.6 mL/min/kg, 3906.2 mL/kg for Tigecycline in formulation (60 mg/mL pyruvate, 3mg/mL ascorbic acid, pH 7 in saline) , respectively1.Animal Model: NOD/SCID mic

12、e with OCI-AML2 acute myeloid leukemia (AML) xenograft model1Dosage: 50 mg/kgAdministration: Intraperitoneal injection; twice a day; for 11 daysResult: Reduced tumor volume and weight.Animal Model: NOD/SCID mice1Page 2 of 3 www.MedChemEDosage: 50 mg/kgAdministration: Intraperitoneal injection; 360 m

13、inutesResult: The peak plasma concentration (Cmax), the terminal half-life (t1/2), area under theplasma concentration-time curve (AUC), clearance (CL) and volume of distribution(Vz) are 22.8 g/mL, 108.9 min, 1912.2 min*g/mL, 26.1 mL/min/kg, 4109.4 mL/kg,respectively.戶使本產品發表的科研獻 Antimicrob Agents Che

14、mother. 2019 May 24;63(6). pii: e00470-19. Int J Antimicrob Agents. 2018 Aug;52(2):269-271.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May28;9(5):e95281.2. Falagas ME, et al. Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals. Int JAntimicrob Agents. 2018 Aug;52(2):269-271.