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  3. Tigecycline

Tigecycline (Synonyms: GAR-936)

Cat. No.: HY-B0117 Purity: 99.88%
Handling Instructions

Tigecycline (GAR-936) 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.

For research use only. We do not sell to patients.

Tigecycline Chemical Structure

Tigecycline Chemical Structure

CAS No. : 220620-09-7

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Based on 2 publication(s) in Google Scholar

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Description

Tigecycline (GAR-936) is a broad-spectrum glycylcycline antibiotic. The mean inhibitory concentration (MIC) of Tigecycline for E. coli (MG1655 strain) is approximately 125 ng/mL[1]. MIC50 and MIC90 are 1 and 2 mg/L for Acinetobacter baumannii (A. baumannii), respectively[2].

IC50 & Target

Mean MIC: 125 ng/mL (E. coli)[1]
MIC50: 1 mg/mL (A. baumannii)[2]
MIC90: 2 mg/mL (A. baumannii)[2]

In Vitro

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[1].

Cell Viability Assay[1]

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).
In Vivo

Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) reduces tumor volume and weight in NOD/SCID mice[1].
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 22.8μg/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 (Cmax), the terminal half-life (t1/2), 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[1].

Animal Model: NOD/SCID mice with OCI-AML2 acute myeloid leukemia (AML) xenograft model[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; twice a day; for 11 days
Result: Reduced tumor volume and weight.
Animal Model: NOD/SCID mice[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 360 minutes
Result: 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.
Clinical Trial
Molecular Weight

585.65

Formula

C₂₉H₃₉N₅O₈

CAS No.

220620-09-7

SMILES

O=C(C(C1=O)=C(O)[[email protected]@H](N(C)C)[[email protected]]2([H])C[[email protected]]3([H])CC4=C(C(C3=C(O)[[email protected]@]21O)=O)C(O)=C(NC(CNC(C)(C)C)=O)C=C4N(C)C)N

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (256.13 mM; Need ultrasonic)

H2O : 50 mg/mL (85.38 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.27 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.88%

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Tigecycline
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