Tigecycline (tetramesylate)

GAR-936 tetramesylate

C33H55N5O20S4

DMSO : 100 mg/mL (103.09 mM; Need ultrasonic); H2O : 50 mg/mL (51.54 mM; Need ultrasonic)

Anti-infection; Autophagy

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 uM, 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 uM (freshly prepared). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s of 5.64+/-0.55 and 4.27+/-0.45 uM (1 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s of 5.02+/-0.60 and 4.39+/-0.44 uM (2 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC₅₀s of 4.09+/-0.41 and 3.95+/-0.39 uM (3 day preincubation). After a 4 day preincubation of Tigecycline in saline, Tigecycline lost its ability to kill TEX human leukemia cells (from IC₅₀ca.5 uM when freshly prepared to IC₅₀>50 uM after 4 days preincubation) as measured by CellTiter Flour assay^[1]. 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 22.8ug/mL, 108.9 min, 1912.2min*ug/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) are15.7ug/mL, 110.3 min, 2036.5 min*ug/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.