Contezolid acefosamil sodium MRX-4 sodium|cas:1807365-35-0|西域试剂

Contezolid acefosamil sodium MRX-4 sodium,99.38%

产品编号：Bellancom-19915B| CAS NO：1807365-35-0| 分子式：C₂₀H₁₇F₃N₄NaO₈P| 分子量：552.33

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-19915B		￥9200.00	杭州北京（现货）
Bellancom-19915B		￥14500.00	杭州北京（现货）

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Contezolid acefosamil sodium 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 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).

体外研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 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.

体内研究

西域 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.

性状

Solid

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 mg	5 mg	10 mg

1 mM	1.8105 mL	9.0526 mL	18.1051 mL
5 mM	0.3621 mL	1.8105 mL	3.6210 mL
10 mM	0.1811 mL	0.9053 mL	1.8105 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°C, 6 months (stored under nitrogen)。-80°C 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-CD in 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 μL 20% 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。