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1135871-27-0

中文名称 1135871-27-0
英文名称 Tigecycline (Mesylate)
CAS 1135871-27-0
分子式 C30H43N5O11S
分子量 681.754
MOL 文件 1135871-27-0.mol
1135871-27-0 结构式 1135871-27-0 结构式

基本信息

中文别名
甲磺酸替加环素
英文别名
Tigecycline (Mesylate)

物理化学性质

储存条件-20°C储存
溶解度溶于二甲基亚砜
形态粉末

常见问题列表

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 )

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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