Contezolid

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Contezolid

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。

CAS NO:

1112968-42-9

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-I

产品介绍

Contezolid (MRX-I) 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 (MRX-I) 可显著降低骨髓移植和单胺氧化酶抑制。

生物活性

Contezolid (MRX-I), a new and orally activeoxazolidinone, is anantibioticin study for complicated skin and soft tissue infections (cSSTI) caused by resistant Gram-positive bacteria. Contezolid (MRX-I) 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 C_max/dose was 524, 1065, and 259 ng/mL/(mg/kg); dose-normalized AUC_0–t/dose was 1654, 3703, and 1664 ngoh/mL/(mg/kg); T_1/2is 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

408.33

性状

Solid

Formula

C₁₈H₁₅F₃N₄O₄

CAS 号

1112968-42-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

溶解性数据

In Vitro:

DMSO : 120 mg/mL(293.88 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.4490 mL	12.2450 mL	24.4900 mL
5 mM	0.4898 mL	2.4490 mL	4.8980 mL
10 mM	0.2449 mL	1.2245 mL	2.4490 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; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 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: ≥ 2.08 mg/mL (5.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.09 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.09 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (5.09 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.09 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 20.8 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。