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Cat #: V3708 CAS #: 856867-39-5 Purity ≥ 98%
Description: Tedizolid phosphate disodium (DA-7157; TR-700; DA7157; TR700; torezolid; Sivextro) is the disodium salt of Tedizolid phosphate which is the phosphate ester prodrug of tedizolid. Tedizolid was approved in 2014 by FDA to treat acute bacterial skin and skin structure infections.
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Molecular Weight (MW) | 494.29 |
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Molecular Formula | C17H14FN6Na2O6P |
CAS No. | 856867-39-5 |
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 | |
Synonyms | Tedizolid phosphate disodium salt; Torezolid phosphate sodium salt; DA 7218 phosphate sodium salt; TR 701 phosphate sodium salt; TR-701 phosphate sodium salt |
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 |
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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. |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 2.0231 mL | 10.1155 mL | 20.2310 mL | 40.4621 mL |
5mM | 0.4046 mL | 2.0231 mL | 4.0462 mL | 8.0924 mL |
10mM | 0.2023 mL | 1.0116 mL | 2.0231 mL | 4.0462 mL |
20mM | 0.1012 mL | 0.5058 mL | 1.0116 mL | 2.0231 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.