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Zosurabalpin (Synonyms: Abx MCP; RG6006)

Katalog-Nr.GC75345 Copy One-Click Copy Product Info

Zosurabalpin is a novel class of tethered macrocyclic peptide antibiotics active against various Acinetobacter baumannii complex (ABC) isolates with the MIC90 values of 0.06-0.5mg/L.

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Zosurabalpin Chemische Struktur

Cas No.: 2379336-76-0

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1 mg
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5 mg
518,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of Zosurabalpin

Zosurabalpin is a novel class of tethered macrocyclic peptide antibiotics active against various Acinetobacter baumannii complex (ABC) isolates with the MIC90 values of 0.06-0.5mg/L [1]. Zosurabalpin disrupts the transport of lipopolysaccharide (LPS) by inhibiting the LptB2FGC protein complex, which causes LPS to accumulate to toxic levels inside the cell, ultimately resulting in bacterial death[2]. Zosurabalpin has been widely used to inhibit the proliferation of drug-resistant bacteria in animal models[3].

In vivo, Zosurabalpin treatment via subcutaneous injection at a dose of 60mg/kg every 6 hours for 24 hours significantly reduced bacterial burden and improved survival in a mouse model of A. baumannii-induced pneumonia[4].

References:
[1] Arshad N, Azzam W, Zilberberg M D, et al. Acinetobacter baumannii complex infections: new treatment options in the antibiotic pipeline[J]. Microorganisms, 2025, 13(2): 356.
[2] Wang W J, Dong X M, Li G B. Macrocyclic peptides: up-and-coming weapons to combat antimicrobial resistance[J]. Signal Transduction and Targeted Therapy, 2024, 9(1): 81.
[3] Que W, Deng Z, Gao J. Clinical crusade: zosurabalpin's charge against antibiotic resistance[J]. Trends in Molecular Medicine, 2024, 30(5): 420-422.
[4] Zampaloni C, Mattei P, Bleicher K, et al. A novel antibiotic class targeting the lipopolysaccharide transporter[J]. Nature, 2024, 625(7995): 566-571.

Protocol of Zosurabalpin

Animal experiment [1]:

Animal models

Male CD-1 mice

Preparation Method

Neutropenia was induced in male CD-1 mice by two consecutive intraperitoneal injections of cyclophosphamide monohydrochloride (CPM) on days -4 and -1, respectively, prior to the initiation of treatment with Zosurabalpin. Approximately 106CFU of bacterial suspension of A. baumannii isolate was injected into each thigh muscle to induce infection, and treatment was started 2h after infection. Zosurabalpin (60mg/kg) was administered subcutaneously every 6 hours. The thigh bacterial burden was determined 24h after treatment.

Dosage form

60mg/kg; every 6 hours for 24h; s.c.

Applications

Zosurabalpin treatment of mice resulted in a remarkable decrease in bacterial burden.

References:
[1] Zampaloni C, Mattei P, Bleicher K, et al. A novel antibiotic class targeting the lipopolysaccharide transporter[J]. Nature, 2024, 625(7995): 566-571.

Chemical Properties of Zosurabalpin

Cas No. 2379336-76-0 SDF
Überlieferungen Abx MCP; RG6006
Formula C43H50N8O5S M.Wt 790.97
Löslichkeit DMSO: 4.76 mg/mL (6.02 mM; adjust pH to 7 with 1 M HCL) Storage -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Zosurabalpin

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 1.2643 mL 6.3214 mL 12.6427 mL
5 mM 252.9 μL 1.2643 mL 2.5285 mL
10 mM 126.4 μL 632.1 μL 1.2643 mL
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In vivo Formulation Calculator (Clear solution) of Zosurabalpin

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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