CAS: 197922-42-2; Teduglutide
该化合物是一种合成的人类甘蓝类酸二(GLP-2),一种用于调节肠道生长和功能的荷尔蒙,主要用于治疗短肠综合症,这是手术切除大量肠道后可能出现的一种症状.Teduglutide提倡肠胃吸收营养和液体,从而改善有这种症状的病人的生活质量.该物质是通过下皮注射方式施用的,由于抗酶退化,其半衰期相对较长.其行动机制与GLP-2受体相关,导致肠胃肌肉生长增强,胆囊高度提高,营养吸收改善.常见的副作用可能包括胃肠症状,如腹部和腹部疼痛,以及肿瘤因其生长刺激效应而可能带来的潜在风险.
- 英文名称Teduglutide
- 中文名称替度鲁肽
- IUPAC名称(2S)-2-[[(2S,3R)-2-[[(2S,3S)-2-[[(2S)-6-amino-2-[[(2S,3R)-2-[[(2S)-5-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S,3S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S,3S)-2-[[(2S,3R)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[2-[[(2S)-2-amino-3-(1H-imidazol-5-yl)propanoyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]acetyl]amino]-3-hydroxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxypropanoyl]amino]-3-carboxypropanoyl]amino]-4-carboxybutanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-oxobutanoyl]amino]-3-hydroxybutanoyl]amino]-3-methylpentanoyl]amino]-4-methylpentanoyl]amino]-3-carboxypropanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]propanoyl]amino]propanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-carboxypropanoyl]amino]-3-phenylpropanoyl]amino]-3-methylpentanoyl]amino]-4-oxobutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]amino]-3-methylpentanoyl]amino]-5-oxopentanoyl]amino]-3-hydroxybutanoyl]amino]hexanoyl]amino]-3-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]butanedioic acid
- 其它别名Gattex; Glucagon-Like Peptide Ii [2-Glycine] (Human); Teduglutide; Revestive
- CAS编号197922-42-2
- MFCD编号:MFCD34789752
- EINECS号:812-261-5
- 分子式:C164H252N44O55S分子量:3752.14
- 产品CID: 1007216
- 产品分类原料药 → 激素及调节内分泌功能类药
- 相似结构搜索
- InChIKey: CILIXQOJUNDIDU-ASQIGDHWSA-N
- CILIXQOJUNDIDU-ASQIGDHWSA-N
- 计算化学: 氢键受体数*氢键供体数*可旋转键数*
物理性质
MSDS等安全信息
- 危险描述Not Classified
Reported as not meeting GHS hazard criteria by 1 of 1 companies. For more detailed information, please visit ECHA C&L website. - 安全声明IDENTIFICATION AND USE: Teduglutide is a biosynthetic (recombinant DNA origin) analog of human glucagon-like peptide-2 (GLP-2), a pleiotropic hormone that enhances intestinal mucosal growth and affects intestinal function. It is indicated for the treatment of adult patients with short bowel syndrome (SBS) who are dependent on parenteral support. HUMAN EXPOSURE AND TOXICITY: Based on the pharmacologic activity and findings in animals, the drug has the potential to cause hyperplastic changes including neoplasia. In clinical studies, GI tract polyps (e.g., colorectal, duodenal, and peristomal polyps, including hyperplastic polyps and villous adenomas) have been detected in patients receiving the drug. Malignancies have been reported in several patients receiving teduglutide, including metastatic adenocarcinoma of unconfirmed origin in a patient who had received prior abdominal irradiation for Hodgkin lymphoma and lung cancer (squamous and non-small cell carcinoma) in 2 patients with a history of smoking. ANIMAL STUDIES: In a 2-year carcinogenicity study in rats at subcutaneous doses of 3, 10 and 35 mg/kg/day (about 60, 200 and 700 times the recommended daily human dose of 0.05 mg/kg, respectively), teduglutide caused statistically significant increases in the incidences of adenomas in the bile duct and jejunum of male rats. In a 2-year carcinogenicity study in mice at subcutaneous doses of 1, 3.5 and 12.5 mg/kg/day (about 20, 70 and 250 times the recommended daily human dose of 0.05 mg/kg, respectively), teduglutide caused a significant increase in papillary adenomas in the gall bladder; it also caused adenocarcinomas in the jejunum in male mice at the high dose of 12.5 mg/kg/day (about 250 times the recommended human dose). In animal studies, no effects on embryo-fetal development were observed in pregnant rats given subcutaneous teduglutide at doses up to 50 mg/kg/day (about 1000 times the recommended daily human dose of 0.05 mg/kg) or pregnant rabbits given subcutaneous doses up to 50 mg/kg/day (about 1000 times the recommended daily human dose of 0.05 mg/kg). A pre- and postnatal development study in rats showed no evidence of any adverse effect on pre- and postnatal development at subcutaneous doses up to 50 mg/kg/day (about 1000 times the recommended daily human dose of 0.05 mg/kg). Teduglutide at subcutaneous doses up to 50 mg/kg/day (about 1000 times the recommended daily human dose of 0.05 mg/kg) was found to have no adverse effect on fertility and reproductive performance of male and female rats. Teduglutide was negative in the Ames test, chromosomal aberration test in Chinese hamster ovary cells, and in vivo mouse micronucleus assay.
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2905122000-异丙醇
2905399002-1,4-丁二醇
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专利信息
专利号:US-2024067694-A1
优先权日:2021-01-04
标 题:Synthesis of teduglutide
发明人：GANGA RAMU VASANTHAKUMAR; PATIL NITIN; SUVARNA DEEPA SHANKAR
权利人:BIOCON LTD
摘要:The present invention provides for novel synthetic approach of solid phase synthesis of peptides with C-terminal Aspartic acid by anchoring the side chain carboxylic group of aspartic acid to the solid support to avoid the formation of various impurities and thus resulting in higher yield and ease the purification process. The present invention further provides the usage of free amino acids and reducing agents as antioxidants in the cleavage cocktail to negate the formation of oxidative impurities formed during the global cleavage and isolation of the peptide from solid support.
专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-10150803-B2
优先权日:2016-10-27
标 题:Method of preparing glucagon-like peptide-2 (GLP-2) analog
发明人：CHEN SHIH-LIN; HSIUNG TING-YU
权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD; CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
摘要:The present invention relates a method of preparing a Glucagon-like peptide 2 (GLP-2) analog by gene recombination. The present invention provides an expression vector, which includes: (a) a nucleic acid sequence encoding tag protein; (b) a nucleic acid sequence encoding Smt3 protein (SEQ ID NO: 1); and (c) a nucleic acid sequence encoding linker peptide (SEQ ID NO: 2) and GLP-2 analog. The fusion protein expressed by the expression vector can be cleaved by thrombin, wherein the cleaving position is at the linker peptide, and then the GLP-2 analog is produced.
专利号:US-9695214-B2
优先权日:2013-03-15
标 题 :Solid phase peptide synthesis processes and associated systems
发明人：SIMON MARK DAVID; PENTELUTE BRADLEY L; ADAMO ANDREA; HEIDER PATRICK LOUIS; JENSEN KLAVS F
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis.
专利号:CN-114981285-A
优先权日:2020-12-26
标 题 :Synthesis of C-terminal Protected Fragments of Peptides
专利号:US-10919882-B2
优先权日:2019-05-09
标题:Compounds for use in synthesis of peptidomimetics
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品牌试剂参考报价(招募中)
📌 第三方产品分析报告
合成参考文献
摘要:NIH; DailyMed. Current Medication Information for Gattex (teduglutide) Injection, Powder, Lyophilized, for Solution (Updated: April 2016). Available from, as of July 8, 2016:
参考文献:10.1007/s00520-006-0052-7
摘要:von Bültzingslöwen I, Brennan MT, Spijkervet FK, Logan R, Stringer A, Raber-Durlacher JE, Keefe D. Growth factors and cytokines in the prevention and treatment of oral and gastrointestinal mucositis. Support Care Cancer. 2006 Jun;14(6):519–27. doi: 10.1007/s00520-006-0052-7.
参考文献:10.1016/j.amjsurg.2017.01.018
摘要:Fung JJ. William Hunter Harridge lecture: The changing face of short-gut syndrome management. The American Journal of Surgery. 2017 Mar;213(3):448–51. doi: 10.1016/j.amjsurg.2017.01.018.
参考文献:10.1007/s40268-017-0175-y
摘要:Boudes PF. Risk Evaluation and Mitigation Strategies (REMSs): Are They Improving Drug Safety A Critical Review of REMSs Requiring Elements to Assure Safe Use (ETASU). Drugs in R&D. 2017 Feb 03;17(2):245–54. doi: 10.1007/s40268-017-0175-y.
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