1135871-27-0
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- CAS号:
- 1135871-27-0
- 英文名:
- Tigecycline (Mesylate)
- 英文别名:
- Tigecycline (Mesylate)
- 中文名:
- 1135871-27-0
- 中文别名:
- 甲磺酸替加环素;替加环素甲磺酸盐;化合物 T23460
- CBNumber:
- CB82677040
- 分子式:
- C30H43N5O11S
- 分子量:
- 681.75432
- MOL File:
- 1135871-27-0.mol
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1135871-27-0化学性质
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Powder
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1135871-27-0性质、用途与生产工艺
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。
Mean MIC: 125 ng/mL (
E. coli
)
MIC50: 1 mg/mL (
A. baumannii
)
MIC90: 2 mg/mL (
A. baumannii
)
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:
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Human leukemic OCI-AML2, HL-60 (ATCC) and TEX cell lines
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Concentration:
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0.63-30 µM
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Incubation Time:
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Preincubated for 4 days, treated for 72 hours
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Result:
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Inhibited AML2 cells and HL-60 cells with IC
50
s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared).
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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:
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NOD/SCID mice with OCI-AML2 acute myeloid leukemia (AML) xenograft model
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Dosage:
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50 mg/kg
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Administration:
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Intraperitoneal injection; twice a day; for 11 days
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Result:
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Reduced tumor volume and weight.
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Animal Model:
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NOD/SCID mice
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Dosage:
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50 mg/kg
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Administration:
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Intraperitoneal injection; 360 minutes
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Result:
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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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1135871-27-0
上下游产品信息
上游原料
下游产品
1135871-27-0, 1135871-27-0 相关搜索:
- C30H43N5O11S
- 替加环素甲磺酸盐
- 化合物 T23460
- 甲磺酸替加环素
- 1135871-27-0
- Tigecycline (Mesylate)