CAS: 20449-79-0; Melittin

该化合物是一种源自蜜蜂毒液(Apis mellifera)的peptide,以其强大的生物活动著称,由26个氨基酸组成,分子重量约为2846 Da.美利廷的特征是其两栖病原性,它能够与脂质薄膜相互作用,导致膜干扰和细胞解析.这种属性使它在各个领域,包括免疫学和癌症研究领域引起兴趣,因为它显示出抗微生物和抗癌症活动.此外,美利廷可以引起炎症,并被研究其潜在的治疗用途,尽管其细胞毒性影响需要在医疗用途中仔细考虑. 酸在水中可溶,在薄膜环境中呈现出一种 helical结构,有助于其在脂质双层中形成. 总的来说,麦利廷是了解百万胺相互作用的宝贵模型,并有望开发新的治疗剂.

结构式图片

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上下游产品

N-(fluoren-9-ylmethoxycarbonyl)glycine Fm°C-Val-OH Fm°C-Leu-OH N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-alanine4-(4-ethoxy-4-oxobutoxy)benzoic acid 4-(4-hydroxy-phenoxy)-butyric acid ethyl ester

合成工艺路线路线简述

  • 合成目标产物 Melittin 主要起始原料 Fmoc-Gly-Oh And Fmoc-L-Valine And Fmoc-Leu-Oh And Fmoc-Ala-Oh And Fmoc-Pro-Oh And Fmoc-Ile-Oh And Nalpha-Fmoc-L-Tryptophan And 2-(9H-Fluoren-9-Ylmethoxycarbonylamino)-3-Hydroxy-Butanoic Acid And Fmoc-Lys-Oh And Fmoc-L-Serine And Nalpha-Fmoc-L-Glutamine And Fmoc-L-Arginine
  • (文献来源)合成步骤主要原料 Fmoc-Gly-Oh 和 Fmoc-L-Valine 和 Fmoc-Leu-Oh 和 Fmoc-Ala-Oh 和 Fmoc-Pro-Oh 和 Fmoc-Ile-Oh 和 Nalpha-Fmoc-L-Tryptophan 和 2-(9H-Fluoren-9-Ylmethoxycarbonylamino)-3-Hydroxy-Butanoic Acid 和 Fmoc-Lys-Oh 和 Fmoc-L-Serine 和 Nalpha-Fmoc-L-Glutamine 和 Fmoc-L-Arginine
Cys Melittin,三(2-羰基乙基)磷盐酸盐 在 2-(N-Morpholino)Ethanesulfonic Acid Sodium Salt体系中,用 水作为反应溶剂,反应 0.5H,以to Yield Final Concentrations Of 10 Mg/Ml Melittin And 20 Mm Mes-Na的收率获得melittin
参考文献:Peptide-Based In Vivo Sirna Delivery System
标题:Peptide-Based In Vivo Sirna Delivery System
摘要:本发明涉及一种用于在体内靶向递送rna干扰(Rnai)多核苷酸至肝细胞的组合物.靶向rnai多核苷酸与共同靶向的蜜蜂毒素递送肽一起给予.递送肽提供膜穿透功能,将rnai多核苷酸从细胞外移动到细胞内.可逆修饰提供递送肽的生理响应性.

海关参考信息

专利信息


专利号:US-7655445-B2
优先权日:2003-11-12
标题 :Methods for synthesis of sulfated saccharides
发明人:ROSENBERG ROBERT D; BALAGURUNATHAN KUBERAN
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:The present invention provides methods, processes and reaction mixtures, which produce sulfated heparosan polysaccharides. This invention also provides methods and reaction mixtures for the synthesis of N-deacetylate N-sulfate derivatives of non-sulfated N-acetyl heparosan (HS) polysaccharides.

专利号:US-8080402-B2
优先权日:2004-02-27
标题:Surface expression method of peptides P5 and Anal3 using the gene encoding poly-gamma-glutamate synthetase
发明人:SUNG MOON-HEE; HONG SEUNG-PYO; LEE JONG-SU; JUNG CHANG-MIN; HAHM KYUNG-SOO; LEE DONG-GUN; PARK YOON KYUNG; KIM CHUL-JOONG; POO HA-RYOUNG
权利人:SUNG MOON-HEE; HONG SEUNG-PYO; LEE JONG-SU; JUNG CHANG-MIN; HAHM KYUNG-SOO; LEE DONG-GUN; PARK YOON KYUNG; KIM CHUL-JOONG; POO HA-RYOUNG; BIOLEADERS CORP; KOREA RES INST OF BIOSCIENCE; CHOSUN UNIVERSITY
摘要:The present invention relates to a method for expressing each of peptide antibiotics P5 3 and Anal3 35 having amphiphilicity and showing antibacterial, antifungal and anticancer activities 61, 63, 65, 67, 69, 71, on the microbial surface, using a vector containing outer membrane protein genes (pgsBCA) that are derived from Bacillus sp. strains and involved in the synthesis of poly-gamma-glutamate. Moreover, the present invention relates to lactic acid-forming bacteria having each of the peptide antibiotics P5 15 and Anal3 43 expressed on their surface, and the use thereof. According to the present invention, the peptide antibiotics can be expressed on the surface of various microorganisms transformed with the surface expression vectors. The inventive method for the surface expression of the peptide antibiotics allows the peptide antibiotics to be mass-produced without a purification process. Thus, the inventive method has very high industrial applicability. Further, the present invention can be applied to other peptide antibiotics besides P5 3 and Anal 3 35.

专利号:US-11845970-B2
优先权日:2016-01-15
标 题:Endo-S2 mutants as glycosynthases, method of making and use for glycoengineering of glycoproteins
发明人:WANG LAI-XI; YANG QIANG; LI TIEZHENG; TONG XIN
权利人:UNIV MARYLAND
摘要:The present invention provides for recombinant Endo-S2 mutants (named Endo-S2 glycosynthases) that exhibit reduced hydrolysis activity and increased transglycosylation activity for the synthesis of glycoproteins wherein a desired sugar chain is added to a fucosylated or nonfucosylated GlcNAc-IgG acceptor. As such, the present invention allows for the synthesis and remodeling of therapeutic antibodies thereby providing for certain biological activities, such as, prolonged half-life time in vivo, less immunogenicity, enhanced in vivo activity, increased targeting ability, and/or ability to deliver a therapeutic agent.

专利号:US-11459380-B2
优先权日:2017-06-29
标 题 :Transglycosylation of endo-S and endo-S mutants for antibody glycosylation remodeling
发明人:WANG LAI-XI; TONG XIN; LI TIEZHENG
权利人:UNIV MARYLAND
摘要:The present invention provides for a one-pot enzymatic approach which does not require removal of the enzyme and purification of the intermediate after deglycosylation step, and the Endo-S treatment is able to do both deglycosylation and transglycosylation. The one-pot strategy of the present invention enables chemoenzymatic synthesis of an azido-tagged N-glycoform of monocloncal antibodies which could be further modified through orthogonal chemical ligation for various applications.

专利号:US-10029014-B2
优先权日:2013-09-10
标题:Synthesis of novel asymmetric bow-tie PAMAM dendrimer-based conjugates for tumor-targeting drug delivery
发明人:OJIMA IWAO; WANG TAO; TENG YU-HAN
权利人:UNIV NEW YORK STATE RES FOUND
摘要:The present disclosure relates to a dendrimer-based conjugate of the formula V m -D-C-D′-(T-F) n , which is useful for tumor targeting drug delivery. The use of asymmetric dendrimers allow for specific targeting as well as synthetic reproducibility.

专利号:US-7592320-B2
优先权日:2001-07-26
标题:Cancer gene therapy based on translational control of a suicide gene
发明人:DEBENEDETTI ARRIGO; DEFATTA ROBERT J
权利人:DEBENEDETTI ARRIGO; DEFATTA ROBERT J
摘要:A novel gene therapy for cancer has been discovered, which unlike most prior approaches, does not require specific knowledge of the cancer cells, but instead targets a general characteristic that distinguishes cancer cells from normal cells, i.e., elevated eIF4E expression. The expression of a toxin or conditional toxin such as HTK is translationally repressed in normal cells by placing a complex 5′ UTR in front of its reading frame. In prototype experiments, this HTK mRNA, a transcriptional product of the BK-UTK vector, was translationally regulated so as to largely inhibit its production in normal murine and human cells, while cancer cells efficiently translated the protein, which a resulting increased sensitivity to GCV. Synthesis of the HTK protein from the BK-UTK vector (containing the 5′ UTR of Fibroblast growth factor-2 (“FGF-2â€?) readily occurred in a panel of murine and human breast carcinoma lines, but not in normal cell lines. Subcutaneous tumors and experimental lung metastases of the breast carcinoma line MM2MT in BALB/c mice were greatly reduced by transfection with the BK-UTK vector, followed by GCV administration. Both the BK-UTK and the BK-TK (control) vectors were effective in reducing lung metastasis following systemic delivery of the vectors and subsequent GCV administration. However, the BK-TK vector was highly toxic to mice while little to no toxicity was seen in mice treated with theBK-UTK vector.
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合成参考文献


参考文献:10.1186/1743-422x-8-353
摘要:Metz SW, Geertsema C, Martina BE, Andrade P, Heldens JG, van Oers MM, Goldbach RW, Vlak JM, Pijlman GP. Functional processing and secretion of Chikungunya virus E1 and E2 glycoproteins in insect cells. Virology Journal. 2011 Jul 15;8(1):353. doi: 10.1186/1743-422x-8-353.
参考文献:10.1007/128_2011_188
摘要:Daub CD, Bratko D, Luzar A. Nanoscale wetting under electric field from molecular simulations. Top Curr Chem. 2012;307():155–79. doi: 10.1007/128_2011_188.
参考文献:10.1007/s00249-005-0033-7
摘要:Glättli A, Chandrasekhar I, van Gunsteren WF. A molecular dynamics study of the bee venom melittin in aqueous solution, in methanol, and inserted in a phospholipid bilayer. Eur Biophys J. 2006 Feb;35(3):255–67. doi: 10.1007/s00249-005-0033-7.
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