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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.
| Targets |
Bacterial protein synthesis; FGFR1 (IC50 = 9.3 nM); FGFR2 (IC50 = 7.6 nM); FGFR3 (IC50 = 22 nM); FGFR4 (IC50 = 290 nM)
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| 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 |
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| Additional Infomation |
Tigecycline is tetracycline in which the hydroxy group at position 5 and the methyl group at position 6 are replaced by hydrogen, and with a dimethylamino substituent and an (N-tert-butylglycyl)amino substituent at positions 7 and 9, respectively. A glycylcycline antibiotic, it has activity against a broad range of Gram-positive and Gram-negative bacteria, including tetracycline-resistant organisms. It is used for the intravenous treatment of complicated skin and skin structure infections caused by susceptible organisms. It has a role as an antibacterial drug. It is a member of tetracyclines and a tertiary alpha-hydroxy ketone. It is a conjugate base of a tigecycline(1+).
Tigecycline is a Tetracycline-class Antibacterial. A tetracycline derivative that acts as a protein synthesis inhibitor. It is used as an antibacterial agent for the systemic treatment of complicated skin and intra-abdominal infections. It is also used for the treatment of community-acquired pneumonia. See also: Tigecycline (annotation moved to). |
| Molecular Formula |
C29H39N5O8
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|---|---|
| Molecular Weight |
585.65
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| Exact Mass |
585.279
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| Elemental Analysis |
C, 59.47; H, 6.71; N, 11.96; O, 21.86
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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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| PubChem CID |
54686904
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
890.9±65.0 °C at 760 mmHg
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| Melting Point |
164-166°C
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| Flash Point |
492.6±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.675
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| LogP |
-1.3
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
42
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| Complexity |
1240
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CC(C)(C)NCC(=O)NC1=CC(=C2C[C@H]3C[C@H]4[C@@H](C(=O)C(=C([C@]4(C(=O)C3=C(C2=C1O)O)O)O)C(=O)N)N(C)C)N(C)C
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| InChi Key |
SOVUOXKZCCAWOJ-HJYUBDRYSA-N
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| InChi Code |
InChI=1S/C29H39N5O8/c1-28(2,3)31-11-17(35)32-15-10-16(33(4)5)13-8-12-9-14-21(34(6)7)24(38)20(27(30)41)26(40)29(14,42)25(39)18(12)23(37)19(13)22(15)36/h10,12,14,21,31,36-37,40,42H,8-9,11H2,1-7H3,(H2,30,41)(H,32,35)/t12-,14-,21-,29-/m0/s1
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| Chemical Name |
(4S,4aS,5aR,12aR)-9-[[2-(tert-butylamino)acetyl]amino]-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4H-tetracene-2-carboxamide
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| Synonyms |
GAR-936; GAR936; Tigecycline; 220620-09-7; Tygacil; WAY-GAR-936; GAR-936; 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.
Antibiotic Therapy for Infectious Diseases
CTID: NCT04937894
Phase: Status: Recruiting
Date: 2021-06-24
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Products are for research use only; We do not sell to patients
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