Contezolid (Synonyms: MRX-I)

Name: Contezolid
Brand: MedChemExpress
SKU: HY-19915
Rating: 4.5 (2 reviews)

Cat. No.: HY-19915 Purity: 99.11%: FAQs
Data Sheet SDS COA Handling Instructions

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Contezolid (MRX-I), 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 (MRX-I) markedly reduces potential for myelosuppression and monoamine oxidase inhibition (MAOI).

For research use only. We do not sell to patients.

Contezolid Chemical Structure

CAS No. : 1112968-42-9

Size	Price	Stock	Quantity
5 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 4200	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 6700	In-stock	Estimated Time of Arrival: December 31
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500 mg		Get quote

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Based on 2 publication(s) in Google Scholar

Other Forms of Contezolid:

Contezolid acefosamil sodium In-stock
Contezolid phosphoramidic acid Get quote
Contezolid acefosamil Get quote

2 Publications Citing Use of MCE Contezolid

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Biological Activity
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Description

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].

MedChemExpress (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%^[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].

MedChemExpress (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^[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

Molecular Weight

408.33

Formula

C₁₈H₁₅F₃N₄O₄

CAS No.

1112968-42-9

Appearance

Solid

Color

White to light yellow

SMILES

O=C1CCN(C2=C(F)C=C(N3C(O[C@@H](CNC4=NOC=C4)C3)=O)C(F)=C2F)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility

In Vitro:

DMSO : 120 mg/mL (293.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.37% ee.: 99.28%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (248 KB) HNMR (205 KB) NP-HPLC (432 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4490 mL	12.2450 mL	24.4900 mL	61.2250 mL
	5 mM	0.4898 mL	2.4490 mL	4.8980 mL	12.2450 mL
	10 mM	0.2449 mL	1.2245 mL	2.4490 mL	6.1225 mL
	15 mM	0.1633 mL	0.8163 mL	1.6327 mL	4.0817 mL
	20 mM	0.1224 mL	0.6122 mL	1.2245 mL	3.0612 mL
	25 mM	0.0980 mL	0.4898 mL	0.9796 mL	2.4490 mL
	30 mM	0.0816 mL	0.4082 mL	0.8163 mL	2.0408 mL
	40 mM	0.0612 mL	0.3061 mL	0.6122 mL	1.5306 mL
	50 mM	0.0490 mL	0.2449 mL	0.4898 mL	1.2245 mL
	60 mM	0.0408 mL	0.2041 mL	0.4082 mL	1.0204 mL
	80 mM	0.0306 mL	0.1531 mL	0.3061 mL	0.7653 mL
	100 mM	0.0245 mL	0.1224 mL	0.2449 mL	0.6122 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Contezolid1112968-42-9MRX-IInhibitorinhibitorinhibit

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Contezolid (Synonyms: MRX-I)

Customer Review

Other Forms of Contezolid:

Contezolid Related Antibodies

2 Publications Citing Use of MCE Contezolid

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Contezolid Related Antibodies

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Complete Stock Solution Preparation Table

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