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Contezolid acefosamil sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Contezolid acefosamil sodium图片
CAS NO:1807365-35-0
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品名称
MRX-4 sodium
产品介绍
Contezolid acefosamil sodium (MRX-4) 是一种新型的恶唑烷酮,用于耐药革兰氏阳性菌引起的皮肤组织感染并发症 (cSSTI) 的抗生素。Contezolid acefosamil sodium (MRX-4) 可显著降低骨髓移植和单胺氧化酶抑制。
生物活性

Contezolid acefosamil sodium (MRX-4), a new and orally activeoxazolidinone, is anantibioticin 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 andmonoamine oxidaseinhibition (MAOI)[1][2].

IC50& Target

Oxazolidinone

 

体外研究
(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[2].

体内研究
(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 Cmax/dose was 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC0–t/dose was 1654, 3703, and 1664 ngoh/mL/(mg/kg); T1/2is 1, 1.5, and 3 h; and the oral bioavailability is 69%, 109%, and 37%[2].
Contezolid (MRX-I) exhibits no obvious toxicity[2].
Contezolid (MRX-I, 100 mg/kg, once daily) significantly reduced the bacterial load in lungs compared to the untreated early and late controls[3].

Animal Model:BALB/c mice infected intranasally withM. tuberculosisErdman[3].
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[2].
Dosage:20, 100, and 200/300 mg/kg/day.
Administration:Orally twice daily.
Result:No mortality was observed.
Clinical Trial
分子量

552.33

性状

Solid

Formula

C20H17F3N4NaO8P

CAS 号

1807365-35-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-80°C, stored under nitrogen

溶解性数据
In Vitro: 

DMSO : 180 mg/mL(325.89 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.8105 mL9.0526 mL18.1051 mL
5 mM0.3621 mL1.8105 mL3.6210 mL
10 mM0.1811 mL0.9053 mL1.8105 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months (stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 4.5 mg/mL (8.15 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (8.15 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 4.5 mg/mL (8.15 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (8.15 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 4.5 mg/mL (8.15 mM); Clear solution

    此方案可获得 ≥ 4.5 mg/mL (8.15 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 45.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。