Ciclosporin EP Impurity E NEW

Ciclosporin EP Impurity E;108027-46-9

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E-mail: anna@molcoo.com

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• Product Information

• Product Number: C088011

• English Name: Ciclosporin EP Impurity E

• English Alias: Ciclosporin V; (3S,6S,9S,12R,15S,18S,21S,24S,30S,33S)-15,30-diethyl-33-((1R,2R,E)-1-hydroxy-2-methylhex-4-en-1-yl)-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,19,25,28-octamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29,32-undecaone

• CAS Number: 108027-46-9

• Molecular Formula: C₆₃H₁₁₃N₁₁O₁₂

• Molecular Weight: 1216.64

• Advantages

• As an EP impurity of Ciclosporin, this compound has the following advantages:
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• Well-defined and distinct structure: A cyclic undecapeptide derivative belonging to the ciclosporin family, differing from Ciclosporin A in specific alkyl substituents (e.g., ethyl groups at positions 15 and 30). It can be accurately distinguished by techniques such as UPLC and LC-MS, providing a specific marker for impurity detection;

• High stability and traceability: The cyclic peptide structure is stable under neutral conditions. As a product of amino acid assembly differences in ciclosporin fermentation or synthesis, it directly reflects the selectivity bias of enzyme catalysis in biosynthesis, improving the accuracy of process tracing;

• Outstanding standard reference value: Compliant with European Pharmacopoeia (EP) impurity standards, it can serve as an official reference substance for quality control of ciclosporin APIs and formulations, ensuring the standardization of detection methods and reliability of data.

• Applications

• Pharmaceutical quality control: Used as an EP standard impurity reference in ciclosporin production to identify and quantify Ciclosporin EP Impurity E, ensuring residual structural analogs from fermentation or synthesis meet EP and regulatory requirements;

• Production process optimization: Reducing structural analog formation by monitoring impurity content and optimizing fermentation conditions (e.g., medium composition, fermentation time) or amino acid coupling selectivity in chemical synthesis;

• Pharmacodynamic assessment: Used to study the difference in immunosuppressive activity between Ciclosporin V and Ciclosporin A, providing data support for potential impacts of impurities on drug efficacy.

• Background Description

• Ciclosporin is a potent immunosuppressant used to prevent organ transplant rejection and treat autoimmune diseases, with natural products being mixtures of structural analogs (e.g., Ciclosporin A, B, C, V). Ciclosporin V, with weaker immunosuppressive activity than Ciclosporin A due to different alkyl substitutions, is listed as a controlled specific impurity in the European Pharmacopoeia. Its control is crucial for ensuring the clinical efficacy and safety of ciclosporin.

• Research Status

• Current research focuses on:
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• Detection method optimization: Using UPLC-MS/MS with optimized mass spectrometry parameters based on characteristic amino acid fragment ions (e.g., methylvaline) to achieve trace detection of this impurity (detection limits up to ppb level);

• Biosynthetic mechanism analysis: Clarifying the biosynthesis pathway of Ciclosporin V through gene sequencing of ciclosporin synthetase, providing a theoretical basis for regulation of fermentation product distribution;

• Activity comparison studies: Comparing the inhibitory effect on IL-2 secretion between Ciclosporin V and Ciclosporin A via in vitro T lymphocyte proliferation assays to evaluate impurity impacts on overall immunosuppressive efficacy;

• Purification technology improvement: Developing novel chiral columns or simulated moving bed techniques to enhance separation efficiency between Ciclosporin A and V, reducing impurity level

We can also customize related analogues and modified peptides including HPLC, MS, 1H-NMR, MS, HPLC, IR, UV, COA, MSDS.
This product is intended for laboratory use only!

WhatsAPP: +86 17386083646
E-mail: anna@molcoo.com