Tigecycline tetramesylate 替加环素四甲磺酸盐; GAR-936 tetramesylate|西域试剂

Tigecycline tetramesylate 替加环素四甲磺酸盐; GAR-936 tetramesylate,95.0%

产品编号：Bellancom-B0117C| 分子式：C₃₃H₅₅N₅O₂₀S₄| 分子量：970.07

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货号	价格	库存与货期
Bellancom-B0117C	￥860.00	杭州北京（现货）
Bellancom-B0117C	￥2100.00	杭州北京（现货）
Bellancom-B0117C	￥3600.00	杭州北京（现货）

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Tigecycline tetramesylate 替加环素四甲磺酸盐; GAR-936 tetramesylate

产品介绍

Tigecycline tetramesylate (GAR-936 tetramesylate) 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。

生物活性

Tigecycline tetramesylate (GAR-936 tetramesylate) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline 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.

体外研究

Tigecycline (0.63-30 µM, preincubated for 4 days, treated for 72 h) inhibits AML2 cells and HL-60 cells with IC₅₀s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s of 5.64±0.55 and 4.27±0.45 μM (1 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s of 5.02±0.60 and 4.39±0.44 μM (2 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s 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 IC₅₀~5 µM when freshly prepared to IC₅₀>50 µM after 4 days preincubation) as measured by CellTiter Flour assay.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC₅₀s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared).

体内研究
(In Vivo)

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (103.09 mM; Need ultrasonic)

H₂O : 50 mg/mL (51.54 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.0309 mL	5.1543 mL	10.3085 mL
5 mM	0.2062 mL	1.0309 mL	2.0617 mL
10 mM	0.1031 mL	0.5154 mL	1.0309 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： PBS
Solubility: 50 mg/mL (51.54 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (2.58 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.58 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (2.58 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (2.58 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明