Tedizolid phosphate disodium salt

Molecular Weight (MW)	494.29
Formula	C17H14FN6Na2O6P
CAS No.	856867-39-5 (disodium);
Storage	-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: ≥ 37 mg/mL (80 mM)
Water: ≥ 1 mg/mL
Ethanol: ≥ 1 mg/mL
Chemical Name	2-Oxazolidinone, 3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl)phenyl)-5-((phosphonooxy)methyl)-, disodium salt, (5R)-
Synonyms	Tedizolid phosphate disodium salt; Torezolid phosphate sodium salt; DA 7218 phosphate sodium salt; TR 701 phosphate sodium salt; TR-701 phosphate sodium salt

Molecular Weight (MW)

494.29

Formula

C17H14FN6Na2O6P

CAS No.

856867-39-5 (disodium);

Storage

-20℃ for 3 years in powder form

-80℃ for 2 years in solvent

Solubility (In vitro)

DMSO: ≥ 37 mg/mL (80 mM)

Water: ≥ 1 mg/mL

Ethanol: ≥ 1 mg/mL

Chemical Name

2-Oxazolidinone, 3-(3-fluoro-4-(6-(2-methyl-2H-tetrazol-5-yl)-3-pyridinyl)phenyl)-5-((phosphonooxy)methyl)-, disodium salt, (5R)-

Synonyms

Tedizolid phosphate disodium salt; Torezolid phosphate sodium salt; DA 7218 phosphate sodium salt; TR 701 phosphate sodium salt; TR-701 phosphate sodium salt

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.
Formulation & Dosage	40 mg/kg of body weight, 13.33 mg/kg, 4.44 mg/kg, and 1.48 mg/kg; i.p.
References	Antimicrob Agents Chemother. 2012 Sep;56(9):4713-7.

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.

Formulation & Dosage

40 mg/kg of body weight, 13.33 mg/kg, 4.44 mg/kg, and 1.48 mg/kg; i.p.

References

Antimicrob Agents Chemother. 2012 Sep;56(9):4713-7.

CAS NO:	856867-39-5
规格:	≥98%

包装	价格(元)
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议