1135871-27-0
- CAS号:1135871-27-0
- 英文名:Tigecycline (Mesylate)
- 中文名:1135871-27-0
- CBNumber:CB82677040
- 分子式:C30H43N5O11S
- 分子量:681.75432
- MOL File:1135871-27-0.mol
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 形态 :Powder
1135871-27-0性质、用途与生产工艺
- 生物活性 Tigecycline mesylate (GAR-936 mesylate) 是一种广谱的甘氨酰环素抗生素。Tigecycline 对 E. coli (MG1655 菌株) 的平均抑制浓度 (MIC) 约为 125 ng/ mL。对 Acinetobacter baumannii (A. baumannii) 的 MIC50 和 MIC90 分别为 1 和 2 mg/L。
-
靶点
Mean MIC: 125 ng/mL ( E. coli )
MIC50: 1 mg/mL ( A. baumannii )
MIC90: 2 mg/mL ( A. baumannii )
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体外研究
Tigecycline (0.63-30 µM, preincubated for 4 days, treated for 72 h) inhibits AML2 cells and HL-60 cells with IC 50 s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared). Tigecycline inhibits AML2 cells and HL-60 cells with IC 50 s of 5.64±0.55 and 4.27±0.45 μM (1 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC 50 s of 5.02±0.60 and 4.39±0.44 μM (2 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC 50 s of 4.09±0.41 and 3.95±0.39 μM (3 day preincubation). After a 4 day preincubation of Tigecycline in saline, Tigecycline lost its ability to kill TEX human leukemia cells (from IC 50 ~5 µM when freshly prepared to IC 50 >50 µM after 4 days preincubation) as measured by CellTiter Flour assay.
Cell Viability Assay
Cell Line: Human leukemic OCI-AML2, HL-60 (ATCC) and TEX cell lines Concentration: 0.63-30 µM Incubation Time: Preincubated for 4 days, treated for 72 hours Result: Inhibited AML2 cells and HL-60 cells with IC 50 s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared). -
体内研究
Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) reduces tumor volume and weight in NOD/SCID mice.
The peak plasma concentration (C max ), the terminal half-life (t 1/2 ), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are 22.8μg/mL, 108.9 min, 1912.2min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg for Tigecycline in saline, respectively. The peak plasma concentration (C max ), the terminal half-life (t 1/2 ), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are15.7μg/mL, 110.3 min, 2036.5 min*μg/mL, 24.6 mL/min/kg, 3906.2 mL/kg for Tigecycline in formulation (60 mg/mL pyruvate, 3 mg/mL ascorbic acid, pH 7 in saline) , respectively.Animal Model: NOD/SCID mice with OCI-AML2 acute myeloid leukemia (AML) xenograft model Dosage: 50 mg/kg Administration: Intraperitoneal injection; twice a day; for 11 days Result: Reduced tumor volume and weight. Animal Model: NOD/SCID mice Dosage: 50 mg/kg Administration: Intraperitoneal injection; 360 minutes Result: The peak plasma concentration (C max ), the terminal half-life (t 1/2 ), area under the plasma concentration-time curve (AUC), clearance (CL) and volume of distribution (Vz) are 22.8 μg/mL, 108.9 min, 1912.2 min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg, respectively.
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