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    Autophagy
  2. Bacterial
    Autophagy
    Antibiotic
  3. Tigecycline tetramesylate

Tigecycline tetramesylate (Synonyms: GAR-936 tetramesylate)

Cat. No.: HY-B0117C Purity: 95.36%
Handling Instructions

Tigecycline tetramesylate (GAR-936 tetramesylate) 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 tetramesylate Chemical Structure

Tigecycline tetramesylate Chemical Structure

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 120 In-stock
Estimated Time of Arrival: December 31
100 mg USD 210 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Tigecycline tetramesylate:

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Description

Tigecycline tetramesylate (GAR-936 tetramesylate) 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

970.07

Formula

C₃₃H₅₅N₅O₂₀S₄

SMILES

O=S(C)(O)=O.O=S(C)(O)=O.O=S(C)(O)=O.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.O=S(C)(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (103.09 mM; Need ultrasonic)

H2O : 50 mg/mL (51.54 mM; Need ultrasonic)

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

    Add each solvent one by one:  PBS

    Solubility: 50 mg/mL (51.54 mM); Clear solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (2.58 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (2.58 mM); Clear solution

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

Tigecycline tetramesylateGAR-936 tetramesylateBacterialAutophagyAntibioticInhibitorinhibitorinhibit

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Tigecycline tetramesylate
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HY-B0117C
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