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Gemfibrozil-xenopus glucagon-like peptide-1 derivative and application thereof

A technology of glucagon and Xenopus laevis, which is applied in the direction of glucagon, hormone peptides, specific peptides, etc., can solve the problem of loss of biological activity, etc., to prolong the time of hypoglycemic action, prolong the biological half-life, and improve stability Effect

Active Publication Date: 2020-02-07
南京赛诺生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although natural GLP-1 has many advantages, it faces many problems in its clinical application. It degrades and loses its biological activity. At the same time, GLP-1 is also rapidly filtered by the kidneys, so that its half-life in the body is only about two minutes.

Method used

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  • Gemfibrozil-xenopus glucagon-like peptide-1 derivative and application thereof
  • Gemfibrozil-xenopus glucagon-like peptide-1 derivative and application thereof
  • Gemfibrozil-xenopus glucagon-like peptide-1 derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0062]

[0063] The theoretical relative molecular mass is 4117.6. ESI-MS m / z:calu[M+3H] 3+ 1373.5,[M+4H] 4+ 1030.4;found[M+3H] 3+ 1372.9,[M+4H] 4+ 1029.6.

Embodiment 3

[0065]

[0066] The theoretical relative molecular mass is 4811.3. ESI-MS m / z:calu[M+3H] 3+ 1604.8,[M+4H] 4+ 1203.8;found[M+3H] 3+ 1604.0,[M+4H] 4+ 1203.5.

Embodiment 4

[0068]

[0069] The theoretical relative molecular mass is 4895.5. ESI-MS m / z:calu[M+3H] 3+ 1632.8,[M+4H] 4+ 1224.9;found[M+3H] 3+ 1632.0,[M+4H] 4+ 1224.2.

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Abstract

The invention relates to a gemfibrozil-xenopus glucagon-like peptide-1 derivative. The gemfibrozil modified XenGLP-1 (xenopus glucagon-like peptide-1) derivative is prepared by structurally modifyinga side chain of XenGLP-1, and introducing a micromolecular gemfibrozil derivative with a high serum protein binding rate and a high lipid-lowering effect. The invention provides an application of thederivative in preparation of a medicine and a composition containing the derivative. The XenGLP-1 derivative has high lipid-lowering activity which other GLP-1 medicines do not have, and at the same time, also has high stability, high blood sugar reduction activity and long blood sugar reduction action time.

Description

technical field [0001] The invention relates to a class of Xenopus glucagon-like peptide-1 (XenGLP-1) derivatives and applications thereof Background technique [0002] Diabetes mellitus is a metabolic disease characterized by hyperglycemia and one of the most important chronic non-communicable diseases in the world. Diabetes can be divided into insulin-dependent diabetes (type 1) and non-insulin-dependent diabetes (type 2), of which type 2 diabetes accounts for more than 85% of the number of diabetic patients. According to the latest survey data from the International Diabetes Federation (IDF), the total number of diabetic patients in the world in 2019 was 463 million. It is estimated that by 2045, the number of people with diabetes will reach 700 million. Among them, China is the country with the largest number of patients. In 2019, the number of diabetic patients in China has reached 143 million, which has seriously affected health and social economy. Currently the mos...

Claims

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Application Information

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IPC IPC(8): C07K14/605A61K38/26A61P3/10A61P3/04A61P9/12A61P3/00A61P3/06A61P25/00A61P9/10A61P9/00
CPCC07K14/605A61P3/10A61P3/04A61P9/12A61P3/00A61P3/06A61P25/00A61P9/10A61P9/00A61K38/00
Inventor 韩京陈心雨杨启萌周凤
Owner 南京赛诺生物制药有限公司