计算溶液所需的质量、体积或浓度。
| 活性类型 | Relation | Activity value | Units | Action Type | 期刊 | PubMed Id | doi | Assay Aladdin ID |
|---|
为什么选择此级别
提供 ≥99% 纯度，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
充氩,-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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
规格
别名
康泰唑胺磷酸钠
英文别名
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
规格或纯度
≥99%
英文名称
Contezolid acefosamil sodium
生化机理
Contezolid acefosamil sodium（MRX-4）是一种新型口服活性噁唑烷酮类抗生素，目前正在研究用于治疗由耐药革兰氏阳性细菌引起的复杂皮肤和软组织感染（cSSTI）。Contezolid acefosamil sodium（MRX-4）能显著减少由耐药革兰氏阳性菌引起的复杂皮肤和软组织感染（cSSTI）。
储存条件
充氩,-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
细菌 70S 核糖体抑制剂
纯度
≥99%
名称和识别符
分子类型
小分子
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
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
InChi Key
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
分子量
552.33
技术文档
高级数据
三维结构
交互式化学结构模型
关联靶点（其它种属）
Staphylococcus aureus (210822 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 180 mg/mL (325.89 mM; Need ultrasonic)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥99%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?80 °C、氩气保护条件下保存。本品在氩气保护下供应，每次取用后请在惰性气体下重新密封。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1807365-35-0，分子式为 C20H17F3N4NaO8P，分子量为 552.33 g/mol。InChIKey JANNTEAGZXJITO-BTQNPOSSSA-M。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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