Tigecycline hydrochloride |
| رقم الكتالوجGC16410 |
هيدروكلوريد تيغيسيكلين (GAR-936 هيدروكلوريد) هو مضاد حيوي واسع الطيف للجليسيل سيكلين
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 197654-04-9
Sample solution is provided at 25 µL, 10mM.
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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].
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].
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.
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.
[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.
| Cas No. | 197654-04-9 | SDF | |
| Chemical Name | (4S,4aS,5aR,12aS)-9-((Z)-(2-(tert-butylamino)-1-hydroxyethylidene)amino)-4,7-bis(dimethylamino)-3,10,12,12a-tetrahydroxy-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carbimidic acid hydrochloride | ||
| Canonical SMILES | CC(C)(NC/C(O)=N/C1=CC(N(C)C)=C(C2=C1O)C[C@@](C(C2=O)=C(O)[C@@]34O)([H])C[C@@]3([H])[C@@](N(C)C)([H])C(O)=C(C(O)=N)C4=O)C.Cl | ||
| Formula | C29H40ClN5O8 | M.Wt | 622.11 |
| الذوبان | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6074 mL | 8.0372 mL | 16.0743 mL |
| 5 mM | 0.3215 mL | 1.6074 mL | 3.2149 mL |
| 10 mM | 0.1607 mL | 0.8037 mL | 1.6074 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 33 reference(s) in Google Scholar.)
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