Tigecycline tetramesylate (Synonyms: GAR-936 tetramesylate)

Cat. No.: HY-B0117C: FAQs
Data Sheet SDS Handling Instructions

Molarity Calculator

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

Size	Price	Stock
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	Ask For Quote & Lead Time
Solution
10 mM * 1 mL in DMSO	USD 66	Ask For Quote & Lead Time
Solid
5 mg	USD 38	Ask For Quote & Lead Time
10 mg	USD 60	Ask For Quote & Lead Time
50 mg	USD 120	Ask For Quote & Lead Time
100 mg	USD 210	Ask For Quote & Lead Time

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Tigecycline tetramesylate:

Tigecycline

Other Forms of Tigecycline tetramesylate:

25 Publications Citing Use of MCE Tigecycline tetramesylate

Cell Viability Assay

: Tigecycline tetramesylate purchased from MedChemExpress. Usage Cited in: Microbiol Spectr. 2022 Dec 8;e0323822. [Abstract]; The MIC distributions of Tigecycline against 43 M. fortuitum isolates (incubate for 24 h). The y axis shows the number of strains with each MIC value, with the specific numbers shown above the bars.

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Biological Activity
Purity & Documentation
References
Customer Review

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].

MedChemExpress (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 (C_max), the terminal half-life (t_1/2), 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 (C_max), the terminal half-life (t_1/2), 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.

MedChemExpress (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 (C_max), the terminal half-life (t_1/2), 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

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=S(C)(O)=O.O=S(C)(O)=O.O=S(C)(O)=O.O=C(C(C1=O)=C(O)[C@@H](N(C)C)[C@]2([H])C[C@]3([H])CC4=C(C(C3=C(O)[C@@]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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (103.09 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (51.54 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Data Sheet (284 KB) SDS (251 KB) Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.0309 mL	5.1543 mL	10.3085 mL	25.7713 mL
	5 mM	0.2062 mL	1.0309 mL	2.0617 mL	5.1543 mL
	10 mM	0.1031 mL	0.5154 mL	1.0309 mL	2.5771 mL
	15 mM	0.0687 mL	0.3436 mL	0.6872 mL	1.7181 mL
	20 mM	0.0515 mL	0.2577 mL	0.5154 mL	1.2886 mL
	25 mM	0.0412 mL	0.2062 mL	0.4123 mL	1.0309 mL
	30 mM	0.0344 mL	0.1718 mL	0.3436 mL	0.8590 mL
	40 mM	0.0258 mL	0.1289 mL	0.2577 mL	0.6443 mL
	50 mM	0.0206 mL	0.1031 mL	0.2062 mL	0.5154 mL
DMSO	60 mM	0.0172 mL	0.0859 mL	0.1718 mL	0.4295 mL
	80 mM	0.0129 mL	0.0644 mL	0.1289 mL	0.3221 mL
	100 mM	0.0103 mL	0.0515 mL	0.1031 mL	0.2577 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Tigecycline tetramesylate Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tigecycline tetramesylateGAR-936 tetramesylateBacterialAutophagyAntibioticInhibitorinhibitorinhibit

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