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Purity: ≥98%
Tigecycline (GAR936; GAR-936; TYGACL) is a potent tetracycline antibiotic which is bacteriostatic. It acts as a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.
ln Vitro |
AML2 cells and HL-60 cells are inhibited by tigecycline (0.63-30 μM, pre-eluted for 4 days, treated for 72 hours) with IC50 values of 4.72±0.54 and 3.06±0.85 μM, respectively (freshly produced). Tigecycline inhibits HL-60 cells and AML2 cells with IC50 values of 4.27±0.45 μM and 5.64±0.55 μM, one day prior to bias. With an IC50 of 5.02±0.60 and 4.39±0.44 μM (pre-biased for two days), tigecycline inhibits AML2. The IC50 values for cells and HL-60 cells, respectively, are 4.09±0.41 and 3.95±0.39 μM (pre-diluted for three days). After 4 days of pre-dilution in saline, tigecycline's capacity to suppress bleaching of TEX human cells decreased (from IC50~5 μM when freshly synthesized) to IC50>50 μM by CellTiter Flour Measure [1].
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ln Vivo |
In NOD/SCID mice, tigecycline (50 mg/kg; intraperitoneally; twice daily; for 11 days) reduces tumor volume and weight [1]. In physiological saline, the peak plasma concentration (Cmax), terminal half-life (t1/2), area under the plasma concentration-time curve (AUC), clearance rate (CL), and distribution concentration (Vz) of tigecycline are, respectively, 22.8μg/mL, 108.9 min, 1912.2min*μg/mL, 26.1 mL/min/kg, 4109.4 mL/kg. In tigecycline formulation (60 mg/mL pyruvate, 3 mg/mL ascorbic acid, physiological saline), the peak plasma concentration (Cmax), area under the plasma concentration-time curve (AUC), clearance (CL), and distribution waveform (Vz) are 15.7 μg/mL, 110.3 min, 2036.5 min*μg/mL, 24.6 mL/min/kg, and 3906.2 mL/kg.
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Cell Assay |
Cell Viability Assay[1]
Cell Types: Human leukemia OCI-AML2, HL-60 (ATCC) and TEX cell lines Tested Concentrations: 0.63-30 µM Incubation Duration: 4 days of pre-incubation, 72 hrs (hours) of treatment Experimental Results: Inhibition of AML2 cells and HL- 60 cells, IC50 are 4.72±0.54 and 3.06±0.85 μM respectively (freshly prepared). |
Animal Protocol |
Animal/Disease Models: NOD/SCID Mouse OCI-AML2 acute myeloid leukemia (AML) xenograft model [1]
Doses: 50 mg/kg Route of Administration: intraperitoneal (ip) injection; for 7) [1]. twice (two times) daily; continued for 11 days Experimental Results: Reduction in 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: peak plasma concentration (Cmax), terminal half-life (t1/2), plasma concentration-time The area under the curve (AUC), clearance (CL) and distribution volume (Vz) were all 22.8 μg/108.9 minutes, 1912.2 minutes*μg/ml, 26.1 ml/minute/kg, and 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 |
C29H39N5O8
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Molecular Weight |
585.65
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Exact Mass |
585.27986
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CAS # |
220620-09-7
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Related CAS # |
Tigecycline tetramesylate;Tigecycline hydrochloride;197654-04-9;Tigecycline mesylate;1135871-27-0;Tigecycline hydrate;1229002-07-6;Tigecycline-d9;2699607-86-6
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O([H])[C@@]12C(=C(C(N([H])[H])=O)C([C@]([H])([C@]1([H])C([H])([H])[C@]1([H])C([H])([H])C3=C(C([H])=C(C(=C3C(=C1C2=O)O[H])O[H])N([H])C(C([H])([H])N([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])=O)N(C([H])([H])[H])C([H])([H])[H])N(C([H])([H])[H])C([H])([H])[H])=O)O[H]
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Synonyms |
GAR-936GAR936 GAR936 TYGACL Tigecycline
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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 : ~25 mg/mL (~42.69 mM)
H2O : ~8.33 mg/mL (~14.22 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 36.67 mg/mL (62.61 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 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 |
*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.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01789905 | COMPLETEDWITH RESULTS | Drug: Tigecycline (Tygacil) | Intra-Abdominal Infections Skin Disease, Infectious |
Pfizer | 2013-04-15 | |
NCT02191475 | UNKNOWN STATUS | Drug: glycopeptide plus carbapenem Drug: Haizheng Li Xing ® plus tazocin ® |
Abdominal Infection | Tianjin Medical University Cancer Institute and Hospital |
2014-05 | Phase 2 Phase 3 |
NCT00488488 | COMPLETEDWITH RESULTS | Drug: tigecycline | Infection | Pfizer | 2006-11 | |
NCT02931526 | UNKNOWN STATUS | Drug: Tigecycline | Bacterial Infection Critically Ill |
Zhujiang Hospital | 2016-08 | |
NCT02931526 | UNKNOWN STATUS | Drug: Tigecycline | Bacterial Infection Critically Ill |
Zhujiang Hospital | 2016-08 |
Ascorbic acid and pyruvate stabilize tigecycline in saline solution. Tigecyline (1 mg/mL) was dissolved in saline solution with or without supplementation with various excipients and incubated in the light. Tigecycline concentrations were detected over time by HPLC and expressed as a relative percentage of that detected immediately following fresh dilution in saline ( = 100%). Tigecycline was dissolved in (A) saline with or without 0.6 mg/mL ascorbic acid, 6 mg/mL pyruvate, 50 mg/mL 2-hydroxypropyl-β-cyclodextrin (HPCD), 0.3 U/mL Oxyrase with 20 mM sodium lactate, 6 mg/mL EDTA sodium, 5% (w/v) glucose, 5% (w/v) mannitol, 10% (v/v) ethanol, 10 mM sodium phosphate (Na-PO4) buffer pH 6.9, or 10 mM sodium bicarbonate (Na-HCO3) buffer pH 6.8; (B) saline containing 0–30 mg/mL ascorbic acid; or (C) saline containing 0–300 mg/mL pyruvate; (D) Iscove's modified Dulbecco's medium (IMDM). In all panels, data indicate the mean ± standard deviation of 3 independent experiments.[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. td> |
Tigecycline is stabilized in solution under novel formulation conditions for up to 7 days. Following dissolution in saline or a novel stabilizing formulation containing ascorbic acid (3 mg/mL) and pyruvate (60 mg/mL) in saline, adjusted to pH 7, tigecycline concentrations were detected by HPLC and expressed as a relative percentage of that detected following fresh dilution in saline ( = 100%). (A) Tigecycline (1 mg/mL) dissolved in saline or the novel formulation was incubated under light or dark conditions, demonstrating light sensitivity. (B) Increasing concentrations of tigecycline were dissolved in the novel formulation and incubated in the dark. Tigecycline stability in solution was reduced at concentrations greater than 1 mg/mL. In all panels, data indicate the mean ± standard deviation of 3 independent experiments.[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. td> |
The novel ascorbic acid- and pyruvate-containing formulation displays efficacy in AML cells grown in vivo. (A) Mice were administered 50/kg tigecycline or 50 mg/kg novel tigecycline formulation by intraperitoneal injection and plasma was collected at increasing times after treatment. Plasma tigecycline concentration was determined using HPLC. 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) were evaluated using WinNonlin 6.2.1. Data represent the mean ± standard deviation of a representative experiment with 3 mice per group. Human leukemia OCI-AML2 cells were injected subcutaneously into the flank of NOD/SCID mice. Eleven days after injection, once tumors were palpable, mice were treated with 50 mg/kg of tigecycline, novel formulation of tigecycline, or vehicle controls (saline or formulation) by intraperitoneal injection twice a day for 11 days (n = 9 per group). Tigecycline in each formulation was prepared fresh twice a day. (B) Tumor volume was monitored over time. Eleven days after injection, mice were sacrificed and tumors excised. (C) Tumor weight was measured. ** indicates p<0.01 and * indicates p<0.05 as determined by Tukey's post-test and one-way ANOVA analysis. Lines represent median. (D) Total proteins were extracted and analyzed by immunoblotting for Cox-1, Cox-2 and Cox-4 expression. PVDF membrane was stained with 0.1% Amido Black.[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. td> |