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编 号：F083760
分子式：C29H39N5O8.xH2O
分子式：C29H39N5O8.xH2O
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CAS No: 1229002-07-6
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生物活性：
Tigecycline (GAR-936) hydrate is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline hydrate for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.
体内研究：
替加环素水合物（50 mg/kg；腹腔注射；每天两次；持续 11 天）可减少 NOD/SCID 小鼠的肿瘤体积和重量。替加环素水合物（50 mg/kg；腹腔注射）在小鼠体内的血药峰浓度 (Cmax)、终末半衰期 (t1/2)、血药浓度-时间曲线下面积 (AUC)、清除率 (CL) 和分布体积 (Vz) 分别为 22.8μg/mL, 108.9 min, 1912.2min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg。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 (Cmax), the terminal half-life (t1/2), 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.
体外研究：
替加环素水合物（0.63-30 μM，预孵育 4 d，处理 72 h）抑制 AML2 细胞和 HL-60 细胞增殖，IC50 分别为 4.72 和 3.06 μM（新鲜制备）。
Tigecycline (GAR-936) hydrate is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline hydrate for E. coli (MG1655 strain) is approximately 125 ng/mL. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively.
体内研究：
替加环素水合物（50 mg/kg；腹腔注射；每天两次；持续 11 天）可减少 NOD/SCID 小鼠的肿瘤体积和重量。替加环素水合物（50 mg/kg；腹腔注射）在小鼠体内的血药峰浓度 (Cmax)、终末半衰期 (t1/2)、血药浓度-时间曲线下面积 (AUC)、清除率 (CL) 和分布体积 (Vz) 分别为 22.8μg/mL, 108.9 min, 1912.2min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg。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 (Cmax), the terminal half-life (t1/2), 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.
体外研究：
替加环素水合物（0.63-30 μM，预孵育 4 d，处理 72 h）抑制 AML2 细胞和 HL-60 细胞增殖，IC50 分别为 4.72 和 3.06 μM（新鲜制备）。
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