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Tigecycline hydrochloride (Synonyms: GAR-936 hydrochloride)

Cat. No.: HY-B0117A
Handling Instructions

Tigecycline hydrochloride (GAR-936 hydrochloride) 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 hydrochloride Chemical Structure

Tigecycline hydrochloride Chemical Structure

CAS No. : 197654-04-9

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Description

Tigecycline hydrochloride (GAR-936 hydrochloride) 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.

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

622.11

Formula

C₂₉H₄₀ClN₅O₈

CAS No.

197654-04-9

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.Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Tigecycline hydrochloride
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