[CAS NO. ] Tigecyclinetetramesylate

Name: Tigecyclinetetramesylate
Brand: Arctom Scientific
SKU: HY-B0117C

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PRODUCTS SPECIFICATIONS

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Catalog

HY-B0117C

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MCE

CAS

DESCRIPTION

Overview

MDL	-
Molecular Weight	970.07
Molecular Formula	C33H55N5O20S4
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

For research use only. We do not sell to patients.

13 Publications Citing Use of MCE

Summary

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] . MIC ₅₀ and MIC ₉₀ 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 IC ₅₀ s of 4.72±0.54 and 3.06±0.85 μM (freshly prepared). Tigecycline inhibits AML2 cells and HL-60 cells with IC ₅₀ s of 5.64±0.55 and 4.27±0.45 μM (1 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC ₅₀ s of 5.02±0.60 and 4.39±0.44 μM (2 day preincubation). Tigecycline inhibits AML2 cells and HL-60 cells with IC ₅₀ s 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 IC ₅₀ ~5 µM when freshly prepared to IC ₅₀ >50 µM after 4 days preincubation) as measured by CellTiter Flour assay ^[1] .

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 IC ₅₀ s 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.

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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01401023	Gary E. Stein, Pharm.D.\|Pfizer\|Michigan State University	Diarrhea\|Clostridium Difficile	July 2011	Not Applicable
NCT01560143	Manjunath Prakash Pai\|Pfizer\|University of Michigan	Obesity	March 2012	Phase 4
NCT00575094	Wyeth is now a wholly owned subsidiary of Pfizer	Community-Acquired Infections	November 2007	Phase 3
NCT00719810	Melinta Therapeutics, Inc.	Skin Structure Infections\|Bacterial Skin Diseases\|Staphylococcal Skin Infections	June 2008	Phase 2
NCT00368537	Wyeth is now a wholly owned subsidiary of Pfizer	Skin Diseases, Bacterial	September 2006	Phase 4
NCT00707239	Pfizer	Pneumonia, Bacterial	December 2008	Phase 2
NCT00488761	Wyeth is now a wholly owned subsidiary of Pfizer	Skin Diseases, Infectious	July 2006	Phase 4
NCT01072539	Pfizer	Complicated Skin and Skin Structure Infections\|Complicated Intra-abdominal Infections\|Community-Acquired Bacterial Pneumonia	May 2010
NCT01332786	University Health Network, Toronto\|University of Kansas\|Memorial Sloan Kettering Cancer Center\|University of California, Los Angeles	Acute Myeloid Leukemia	March 2011	Phase 1
NCT00911573	Wyeth is now a wholly owned subsidiary of Pfizer	Skin Diseases\|Infection	August 2011	Phase 3
NCT00136201	Wyeth is now a wholly owned subsidiary of Pfizer	Abdominal Abscess	November 2005	Phase 3
NCT00080496	Wyeth is now a wholly owned subsidiary of Pfizer	Bacterial Pneumonia	July 2003	Phase 3
NCT01342731	Mahidol University	Antibiotic Resistant Infection	July 2011	Phase 4
NCT00683332	Pfizer	Complicated Skin and Skin Structure Infections\|Complicated Intra-abdominal Infections	April 2007
NCT02931526	Zhujiang Hospital	Bacterial Infection\|Critically Ill	August 2016
NCT03962920	Zealand University Hospital	Microbial Disease	May 1, 2020	Not Applicable
NCT01287793	Pfizer	Healthy	January 2011	Phase 1
NCT00230971	Wyeth is now a wholly owned subsidiary of Pfizer	Appendicitis\|Cholecystitis\|Diverticulitis\|Intra-Abdominal Abscess\|Intra-Abdominal Infection\|Peritonitis	October 2005	Phase 4
NCT02573064	Maimónides Biomedical Research Institute of Córdoba	Acinetobacter Infections	January 2010
NCT00081744	Wyeth is now a wholly owned subsidiary of Pfizer	Gram-Positive Bacterial Infections\|Cross Infection	November 2002	Phase 3
NCT00079989	Wyeth is now a wholly owned subsidiary of Pfizer	Gram-Negative Bacterial Infections	December 2003	Phase 3
NCT01721408	Pfizer	Intra-abdominal Infection	November 2012	Phase 4
NCT01132417	King Faisal University	Infections, Bacterial	September 2009
NCT01592032	Clinica Universidad de Navarra, Universidad de Navarra\|University of Navarrra Hospital (Clinica Universitaria)	Catheter-Related Infections\|Bacteremia.	May 2012	Phase 4
NCT00205816	Wyeth is now a wholly owned subsidiary of Pfizer	Bacterial Infections	January 2004	Phase 3
NCT00376324	Wyeth is now a wholly owned subsidiary of Pfizer	Healthy Subjects	September 2006	Phase 1
NCT01789905	Pfizer	Intra-Abdominal Infections\|Skin Disease, Infectious	April 15, 2013
NCT00600600	The University of Texas Health Science Center at Tyler\|Wyeth is now a wholly owned subsidiary of Pfizer	Mycobacterium Abscessus Lung Disease\|Rapidly Growing Mycobacterial Lung Disease	April 2002	Phase 2
NCT00228410	Wyeth is now a wholly owned subsidiary of Pfizer	Skin Diseases, Infectious	November 2002	Phase 3
NCT04208763	Institute of Liver and Biliary Sciences, India	Spontaneous Bacterial Peritonitis	December 20, 2019	Not Applicable
NCT00488306	Wyeth is now a wholly owned subsidiary of Pfizer	Abdominal Abscess	August 2006	Phase 4
NCT00488488	Pfizer	Infection	November 2006
NCT00079976	Wyeth is now a wholly owned subsidiary of Pfizer	Gram-Positive Bacterial Infections\|Staphylococcus Infections\|Vancomycin Resistance\|Methicillin Resistance	October 2003	Phase 3
NCT03950544	Shanghai 10th People´s Hospital	Antibiotic Resistant Infection	January 1, 2019	Early Phase 1
NCT04489459	Al-Azhar University	Treatment of Blood Stream Infections Due to Multidrug-Resistant Klebsiella Pneumoniae	September 21, 2019	Phase 4
NCT00419991	CPL Associates\|Wyeth is now a wholly owned subsidiary of Pfizer	Staphylococcal Infections	January 2007	Phase 4
NCT00614679	University of California, San Diego	End-Stage Renal Disease\|Hemodialysis Catheter-associated Infection	October 2006	Phase 1
NCT00195351	Wyeth is now a wholly owned subsidiary of Pfizer	Appendicitis\|Cholecystitis\|Cross Infection\|Diverticulitis\|Peritonitis	September 2005	Phase 4
NCT00366249	Wyeth is now a wholly owned subsidiary of Pfizer	Bacterial Infections\|Diabetic Foot\|Osteomyelitis	January 2007	Phase 3
NCT01602874	Pfizer	Community Acquired Bacterial Pneumonia\|Complicated Intra-Abdominal Infection	January 2011	Phase 3
NCT00079885	Wyeth is now a wholly owned subsidiary of Pfizer	Community Acquired Pneumonia\|Bacterial Pneumonia\|Cross Infection	November 2003	Phase 3
NCT00406237	Wyeth is now a wholly owned subsidiary of Pfizer	Liver Cirrhosis, Biliary	December 2006	Phase 1
NCT04042077	Menarini Group	Surgical Site Infection	September 25, 2019	Phase 3
NCT00081575	Wyeth is now a wholly owned subsidiary of Pfizer	Community-Acquired Infections\|Bacterial Pneumonia\|Cross Infection	January 2004	Phase 3
NCT04937894	Shandong University\|Shandong Provincial Hospital	Infectious Disease	June 1, 2021
NCT01970371	Achaogen, Inc.\|Department of Health and Human Services	Bloodstream Infections (BSI) Due to CRE\|Hospital-Acquired Bacterial Pneumonia (HABP) Due to CRE\|Ventilator-Associated Bacterial Pneumonia (VABP) Due to CRE\|Complicated Urinary Tract Infection (cUTI) Due to CRE\|Acute Pyelonephritis (AP) Due to CRE	September 16, 2014	Phase 3
NCT00914888	Wyeth is now a wholly owned subsidiary of Pfizer	Community Acquired Bacterial Pneumonia\|Complicated Intra-Abdominal Infection	January 2011	Phase 3
NCT04310930	The University of Queensland\|Australian Government Department of Health and Ageing\|Children´s Hospital Foundation\|Cystic Fibrosis Foundation\|Newcastle University\|Griffith University\|Erasmus Medical Center\|Monash University\|University of Copenhagen\|Hôpital Cochin\|South Australian Health and Medical Research Institute\|University of Melbourne\|James Cook University, Queensland, Australia\|Murdoch Childrens Research Institute	Pulmonary Disease Due to Mycobacteria (Diagnosis)	March 2, 2020	Phase 2\|Phase 3
NCT00827541	Pfizer	Intra-Abdominal Infections\|Skin Disease, Infectious\|Soft Tissues Infections	August 2008

Appearance

Solid

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)

H ₂ O : 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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 50 mg/mL (51.54 mM); Clear solution; Need ultrasonic
2.

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
3.

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

* All of the co-solvents are available by MCE.