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197654-04-9

中文名稱 197654-04-9
英文名稱 Tigecycline Hydrochloride
CAS 197654-04-9
分子式 C29H40ClN5O8
分子量 622.12
MOL 文件 197654-04-9.mol
197654-04-9 結(jié)構(gòu)式 197654-04-9 結(jié)構(gòu)式

基本信息

中文別名
鹽酸替加環(huán)素
英文別名
Tigecycline Hydrochloride
所屬類別
有機(jī)原料:羧酸類化合物及衍生物

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)粉末

常見問題列表

生物活性
Tigecycline hydrochloride (GAR-936 hydrochloride) 是一種廣譜的甘氨酰環(huán)素抗生素。Tigecycline 對 E. coli (MG1655 菌株) 的平均抑制濃度 (MIC) 約為 125 ng/ mL。對 Acinetobacter baumannii (A. baumannii) 的 MIC50 和 MIC90 分別為 1 和 2 mg/L。
靶點(diǎn)

Mean MIC: 125 ng/mL ( E. coli )
MIC50: 1 mg/mL ( A. baumannii )
MIC90: 2 mg/mL ( A. baumannii )

體外研究

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).
體內(nèi)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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