Tigecycline

Research use only, not for human use.

Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.

Tigecycline is bacteriostatic and is a protein synthesis inhibitor by binding to the 30S ribosomal subunit of bacteria and thereby blocking entry of Aminoacyl-tRNA into the A site of the ribosome during prokaryotic translation.(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.(In Vivo):Tigecycline (50 mg/kg; intraperitoneal injection; twice a day; for 11 days) reduces tumor volume and weight in NOD/SCID mice.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.

Cell Viability Assay 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 hoursResult:Inhibited AML2 cells and HL-60 cells with IC50s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared).

Animal Model:NOD/SCID mice with OCI-AML2 acute myeloid leukemia (AML) xenograft modelDosage:50 mg/kgAdministration:Intraperitoneal injection; twice a day; for 11 daysResult:Reduced tumor volume and weight.Animal Model:NOD/SCID miceDosage:50 mg/kgAdministration:Intraperitoneal injection; 360 minutesResult: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.

GAR 936 | Glycylcycline

Microbiology/Virology

ribosome

30S ribosome

Infection

——

220620-09-7

585.65

C29H39N5O8

>98% (HPLC)

Water: 100 mg/mL (170.75 mM); DMSO: 100 mg/mL (170.75 mM)

O=C(C1=C(O)[C@@H](N(C)C)[C@@](C[C@@]2([H])C(C(C3=C(O)C(NC(CNC(C)(C)C)=O)=CC(N(C)C)=C3C2)=O)=C4O)([H])[C@@]4(O)C1=O)N

(4S,4aS,5aR,12aS)-9-(2-(tert-butylamino)acetamido)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years