Tedizolid phosphate

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
500mg	$450	In Stock
1g	$600	In Stock
5g	$1515	In Stock

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Cat #: V3707 CAS #: 856867-55-5 Purity ≥ 98%

Description: Tedizolid phosphate (DA7157; TR700; DA-7157; TR-700; torezolid; Sivextro), the phosphate ester prodrug of tedizolid, is an oxazolidinone-class antibiotic approved in 2014 by FDA for the treatment of acute bacterial skin and skin structure infections. It is an inhibitor of bacterial protein synthesis by binding to the 50S ribosomal subunit of the G+ bacteria.

References: Choi S, et al. Activity of Tedizolid Phosphate (TR-701) in Murine Models of Infection with Penicillin-resistant and Penicillin-sensitive Streptococcus pneumoniae. Antimicrob Agents Chemother. 2012 Jun 19.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	450.32
Molecular Formula	C17H16FN6O6P
CAS No.	856867-55-5
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: ≥ 37 mg/mL (80 mM)r
	Water: ≥ 1 mg/mLr
	Ethanol: ≥ 1 mg/mL
Synonyms	DA7157; TR700; DA-7157; TR-700; TR701-FA; Tedizolid; TR-701-FA; TR 701-FA; Torezolid phosphate. Trade name: Sivextro

Protocol	In Vitro	In vitro activity: Tedizolid (formerly known as torezolid, TR-700, or DA-7157, trade name Sivextro), is an oxazolidinone-class antibiotic against Gram-positive bacteria. The mechanism of action is to inhibit protein synthesis by binding to the 50S ribosomal subunit of the G+ bacteria. Tedizolid phosphate is a phosphate ester prodrug of the active compound tedizolid. It was developed by Cubist Pharmaceuticals, following acquisition of Trius Therapeutics (formerly Dong-A Pharmaceuticals in Korea), and is approved in 2014 by the US-FDA for the treatment of acute bacterial skin and skin structure infections (also known as complicated skin and skin-structure infections (cSSSIs)). Kinase Assay: Tedizolid (0.25 μg/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid against PRSP Cell Assay: Tedizolid (0.25 μg/mL) inhibits all 28 clinical isolates of PRSP, and is 4-fold more potent than linezolid against PRSP
	In Vivo	Male ICR mice (weight, 18 to 20 g) are inoculated intraperitoneally with 1 of 4 PRSP isolates (DR9, DR10, DR11, or DR14) suspended in 10% mucin, to induce a systemic S. pneumoniae infection. The suspension contained sufficient bacteria to kill 100% of untreated control mice. At 1 h postinfection, mice receives a single dose of either tedizolid phosphate or linezolid, and survival is assessed daily for 7 days postinfection. Treatments are delivered both orally and intravenously at each of four doses (40 mg/kg of body weight, 13.33 mg/kg, 4.44 mg/kg, and 1.48 mg/kg), with 8 mice per group defined by dose, delivery method, and infecting strain. The 50% effective dose (ED50), i.e., the dose allowing survival of 50% of the infected mice, is calculated for each delivery route using probit analysis.
	Animal model	Male ICR mice (weight, 18 to 20 g) are inoculated intraperitoneally with 1 of 4 PRSP isolates (DR9, DR10, DR11, or DR14) suspended in 10% mucin, to induce a systemic S. pneumoniae infection.
	Dosages	40 mg/kg of body weight, 13.33 mg/kg, 4.44 mg/kg, and 1.48 mg/kg
	Administration	i.p.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Related Biological Data

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.2206 mL	11.1032 mL	22.2064 mL	44.4129 mL
5mM	0.4441 mL	2.2206 mL	4.4413 mL	8.8826 mL
10mM	0.2221 mL	1.1103 mL	2.2206 mL	4.4413 mL
20mM	0.1110 mL	0.5552 mL	1.1103 mL	2.2206 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.