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体外研究 (In Vitro) |
Tigecycline 水合物(0.63-30 μM,预孵育 4 天,处理 72 小时)抑制新鲜产生的 AML2 和 HL-60 细胞的生长,IC50 值分别为 4.72 和 3.06 μM。
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体内研究 (In Vivo) |
在 NOD/SCID 小鼠中,替加环素水合物(50 mg/kg;腹腔注射;每天两次;持续 11 天)可减少肿瘤体积和重量 [1]。替加环素水合物(50 mg/kg;腹腔注射):血浆峰浓度(Cmax)、终末半衰期(t1/2)、血药浓度-时间曲线下面积(AUC)、小鼠清除率(CL)分布体积(Vz)分别为22.8μg/mL、108.9 min、1912.2min*μg/mL、26.1 mL/min/kg和4109.4 mL/kg[1]。
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细胞实验 |
细胞活力测定[1]
细胞类型:人类白血病 OCI-AML2、HL-60 (ATCC) 和 TEX 细胞系 测试浓度: 0.63 - 30 µM 孵育时间:预孵育 4 天,处理 72 小时 实验结果:抑制 AML2 细胞和 HL-60 细胞,IC50 4.72 和 3.06 μM(新鲜制备)。 |
动物实验 |
Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse with OCI-AML2 acute myeloid leukemia (AML) xenograft model[1]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip)injection; twice a day; for 11 days Experimental Results: diminished tumor volume and weight. Animal/Disease Models: NOD/SCID (severe combined immunodeficient) mouse[1] Doses: 50 mg/kg Route of Administration: intraperitoneal (ip)injection; 360 minutes Experimental Results: 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. |
参考文献 |
[1]. Jitkova Y, et al. A novel formulation of tigecycline has enhanced stability and sustained antibacterial and antileukemic activity. PLoS One. 2014 May 28;9(5):e95281.
[2]. Falagas ME, et al. Activity of TP-6076 against carbapenem-resistant Acinetobacter baumannii isolates collected from inpatients in Greek hospitals. Int J Antimicrob Agents. 2018 Aug;52(2):269-271. |
分子式 |
C29H39N5O8.XH2O
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分子量 |
585.648667573929
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CAS号 |
1229002-07-6
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相关CAS号 |
Tigecycline;220620-09-7;Tigecycline tetramesylate;Tigecycline hydrochloride;197654-04-9;Tigecycline mesylate;1135871-27-0
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SMILES |
O[C@@]12C(=C(C(N)=O)C([C@H]([C@@H]1C[C@@H]1CC3C(=CC(=C(C=3C(=C1C2=O)O)O)NC(CNC(C)(C)C)=O)N(C)C)N(C)C)=O)O
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溶解度 (体内) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
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制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7075 mL | 8.5375 mL | 17.0750 mL | |
5 mM | 0.3415 mL | 1.7075 mL | 3.4150 mL | |
10 mM | 0.1708 mL | 0.8538 mL | 1.7075 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。