Size | Price | Stock | Qty |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
Mean MIC: 125 ng/mL (E. coli)[1] MIC50: 1 mg/mL (A. baumannii)[2] MIC90: 2 mg/mL (A. baumannii)[2]
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ln Vitro |
With IC50s of 4.72±0.54 and 3.06±0.85 μM (freshly generated), tigecycline (0.63-30 µM, preincubated for 4 days, administered for 72 hours) inhibits AML2 cells and HL-60 cells. After one day of preincubation, tigecycline inhibits HL-60 and AML2 cells with IC50 values of 4.27±0.45 and 5.64±0.55 μM, respectively. 60 cells exhibited 3.95±0.39 μM and 4.09±0.41 μM IC50s (three days preincubation). Tigecycline reduced its capacity to kill TEX human leukemia cells after 4 days of preincubation in saline, as shown by the CellTiter Flour assay. IC50~5 µM when freshly synthesized to IC50 >50 µM after 4 days of preincubation[1].
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ln Vivo |
In NOD/SCID mice, tigecycline (50 mg/kg) administered intraperitoneally twice a day for 11 days decreases tumor mass and volume[1]. Tigecycline in saline has the following values: peak plasma concentration (Cmax), terminal half-life (t1/2), area under the plasma concentration-time curve (AUC), clearance (CL), and volume of distribution (Vz), in that order: 22.8μg/mL, 108.9 min, 1912.2min*μg/mL, 26.1 mL/min/kg, and 4109.4 mL/kg. For Tigecycline in formulation (60 mg/mL pyruvate, 3 mg/mL ascorbic acid, pH 7 in saline), the peak plasma concentration (Cmax), the terminal half-life (t1/2), the area under the plasma concentration-time curve (AUC), the clearance (CL), and the volume of distribution (Vz) are 15.7μg/mL, 110.3 min, 2036.5 min*μg/mL, 24.6 mL/min/kg, and 3906.2 mL/kg, respectively.
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Cell Assay |
Cell Viability Assay[1]
Cell Types: Human leukemic OCI-AML2, HL-60(ATCC) and TEX cell lines Tested Concentrations: 0.63-30 µM Incubation Duration: Preincubated for 4 days, treated for 72 hrs (hours) Experimental Results: Inhibited AML2 cells and HL-60 cells with IC50s of 4.72±0.54 and 3.06±0.85 μM(freshly prepared). |
Animal Protocol |
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: decreased 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. |
References |
[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. |
Molecular Formula |
C33H55N5O20S4
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Molecular Weight |
970.07
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Related CAS # |
Tigecycline;220620-09-7;Tigecycline hydrochloride;197654-04-9;Tigecycline mesylate;1135871-27-0;Tigecycline hydrate;1229002-07-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO :~100 mg/mL (~103.09 mM)
H2O :~50 mg/mL (~51.54 mM) |
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Solubility (In Vivo) |
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  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.