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Contezolid acefosamil sodium - 99%, high purity , Bacterial 70S ribosome inhibitor, CAS No.1807365-35-0, Bacterial 70S ribosome inhibitor

COA

Grade & Purity:

≥99%

Cas Number: 1807365-35-0
Molecular Weight: 552.33
PubChem CID: 131750213

In stock

Item Number

C647354

Grouped product items
SKU	Size	Availability	Price	Qty
C647354-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$920.90
C647354-10mg	10mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$1,450.90

View related series

Antibiotic (1629) Bacterial (3013) Monoamine Oxidase (116) Neuronal Signaling (3320)

Basic Description

Synonyms	Contezolid acefosamil \| HY-19915B \| Prodrug of contezolid (mrx-1) \| 1807365-35-0 \| CHEMBL3989966 \| Contezolid acefosamil [USAN] \| D11298 \| Acetic acid, anhydride with N-(((5R)-3-(4-(3,4-dihydro-4-oxo-1(2H)-pyridinyl)-2,3,5-trifluorophenyl)-2-oxo-5-oxazoli
Specifications & Purity	≥99%
Biochemical and Physiological Mechanisms	Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone , is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduc
Storage Temp	Argon charged,Store at -80°C
Shipped In	Ice chest + Ice pads This product requires cold chain shipping. Ground and other economy services are not available.
Action Type	INHIBITOR
Mechanism of action	Bacterial 70S ribosome inhibitor
Product Description	Contezolid acefosamil sodium (MRX-4), a new and orally active oxazolidinone , is an antibiotic in study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid acefosamil sodium (MRX-4) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI) In Vitro Contezolid (MRX-I) is highly potent against all Grampositive clinical isolates of staphylococci, streptococci, and enterococci, including MDR organisms such as MRSA, methicilline-resistant Streptococcus epidermidis (MRSE), penicillin-resistant Streptococci (PRSP), and VRE. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo Oral absorption of Contezolid (MRX-I) occurrs rapidly in mouse, rat, and dog, with peak plasma concentrations observed at 0.5−2.6 h postdose. In mouse, rat, and dog, respectively, PK parameters are determined as follows: dose-normalized C max /dose was 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC 0−t /dose was 1654, 3703, and 1664 ng•h/mL/(mg/kg); T 1/2 is 1, 1.5, and 3 h; and the oral bioavailability is 69%, 109%, and 37%. Contezolid (MRX-I) exhibits no obvious toxicity. Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: BALB/c mice infected intranasally with M. tuberculosis Erdman. Dosage: 100, 50 (twice), 25 (twice) mg/kg. Administration: Gavage, once or twice daily, five days per week for four weeks. Result: Significantly reduced the CFU recovered from the lungs compared to the early and late control mice (P < 0.05). Twice daily MRX-I at 50mg/kg and 25 mg/kg were significantly better than the late control mice (P < 0.05). Once daily MRX-I at 100 mg/kg was significantly better than twice daily 50 mg/kg and 25 mg/kg (P < 0.05). There was no statistical difference between twice daily 50 mg/kg of MRX-I and 25mg/kg (P > 0.05). Animal Model: Rats. Dosage: 20, 100, and 200/300 mg/kg/day. Administration: Orally twice daily. Result: No mortality was observed. Form:Solid IC50& Target:Oxazolidinone

Mechanisms of Action

Mechanism of Action	Action Type	target ID	Target Name	Target Type	Target Organism	Binding Site Name	References

Names and Identifiers

IUPAC Name	sodium;acetyloxy-[1,2-oxazol-3-yl-[[(5R)-2-oxo-3-[2,3,5-trifluoro-4-(4-oxo-2,3-dihydropyridin-1-yl)phenyl]-1,3-oxazolidin-5-yl]methyl]amino]phosphinate
INCHI	InChI=1S/C20H18F3N4O8P.Na/c1-11(28)35-36(31,32)27(16-4-7-33-24-16)10-13-9-26(20(30)34-13)15-8-14(21)19(18(23)17(15)22)25-5-2-12(29)3-6-25;/h2,4-5,7-8,13H,3,6,9-10H2,1H3,(H,31,32);/q;+1/p-1/t13-;/m1./s1
InChIKey	JANNTEAGZXJITO-BTQNPOSSSA-M
Smiles	CC(=O)OP(=O)(N(C[C@H]1CN(C(=O)O1)C2=CC(=C(C(=C2F)F)N3CCC(=O)C=C3)F)C4=NOC=C4)[O-].[Na+]
Isomeric SMILES	CC(=O)OP(=O)(N(C[C@H]1CN(C(=O)O1)C2=CC(=C(C(=C2F)F)N3CCC(=O)C=C3)F)C4=NOC=C4)[O-].[Na+]
PubChem CID	131750213
Molecular Weight	552.33

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