1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETigecycline hydrochlorideCat. No.: HY-B0117ACAS No.: 197654-04-9Synonyms: GAR-936 hydrochloride分式: CHClNO分量: 622.11作靶點(diǎn): Bacterial; Autophagy作通路: Anti-infection; Autophagy儲(chǔ)存式: Please store the product under the recommended condit

2、ions inthe COA.BIOLOGICAL ACTIVITY物活性 Tigecycline hydrochloride (GAR-936 hydrochloride)種譜的氨酰環(huán)素抗素。Tigecycline 對(duì) E. coli(MG1655菌株) 的平均抑制濃度 (MIC) 約為 125 ng/ mL 1。對(duì) Acinetobacter baumannii (A. baumannii) 的MIC50 和 MIC90 分別為 1 和 2 mg/L 2。IC50 & Target Mean MIC: 125 ng/mL (E. coli) 1MIC50: 1 mg/mL (A. baum

3、annii) 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 withIC50s of 4.720.54 and 3.060.85 M (freshly prepared). Tigecycline inhibits AML2 cells and HL-60 cellswith IC50s of 5.640.55 and 4.270.45 M (1 day prein

4、cubation). Tigecycline inhibits AML2 cells and HL-60cells with IC50s of 5.020.60 and 4.390.44 M (2 day preincubation). Tigecycline inhibits AML2 cells andHL-60 cells with IC50s of 4.090.41 and 3.950.39 M (3 day preincubation). After a 4 day preincubation ofTigecycline in saline, Tigecycline lost its

5、 ability to kill TEX human leukemia cells (from IC505 M whenfreshly prepared to IC5050 M after 4 days preincubation) as measured by CellTiter Flour assay 1.Cell Viability Assay 1Cell Line: Human leukemic OCI-AML2, HL-60 (ATCC) and TEX cell linesConcentration: 0.63-30 M1/3 Master of Small Molecules 您

6、邊的抑制劑師www.MedChemEIncubation Time: Preincubated for 4 days, treated for 72 hoursResult: Inhibited AML2 cells and HL-60 cells with IC50s of 4.720.54 and 3.060.85 M (freshlyprepared).體內(nèi)研究 Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) reduces tumor volume and weight inNOD/

7、SCID mice 1.The peak plasma concentration (Cmax), the terminal 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 pea

8、k plasma concentration(Cmax), the terminal half-life (t1/2), area 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/kgfor Tigecycline in formulation (60 mg/mL pyruvate, 3 mg/mL ascorbic ac

9、id, pH 7 in saline) , respectively.Animal Model: NOD/SCID mice with OCI-AML2 acute myeloid leukemia (AML) xenograft model 1Dosage: 50 mg/kgAdministration: Intraperitoneal injection; twice a day; for 11 daysResult: Reduced tumor volume and weight.Animal Model: NOD/SCID mice 1Dosage: 50 mg/kgAdministr

10、ation: Intraperitoneal injection; 360 minutesResult: 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,respect

11、ively.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Antimicrob Agents Chemother. 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.MedChemEREFERENCES1. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacter

12、ial and antileukemic activity. PLoS2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEOne. 2014 May 28;9(5):e95281.2. Falagas ME, et al. Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greekhospitals. Int J Antimicrob Agents. 2018 Aug;52(2):269-271.McePdfHeightCaution: