CAS: 121062-08-6; Melanotan Ii Acetate Salt

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Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys-Nh2置于dipotassium Hydrogenphosphate,叠氮磷酸二苯酯体系中,用 N,N-二甲基甲酰胺 用作溶剂,以30%的收率获得美拉诺坦 Ii
参考文献:Potent And Prolonged-Acting Cyclic Lactam Analogs Of .Alpha.-Melanotropin: Design Based On Molecular Dynamics
标题:Potent And Prolonged-Acting Cyclic Lactam Analogs Of .Alpha.-Melanotropin: Design Based On Molecular Dynamics
摘要:Utilizing Results From Previous Structure-Activity Relationships And Theoretical Studies Of Alpha-Melanotropin (Alpha-Msh,Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Nh2) And Its Related Superpotent Analogues,Ac-[nle4,D-Phe7]-Alpha-Msh And Ac-[cys4,Cys10]-Alpha-Msh,We Have Designed A New Class Of Alpha-Msh4-13 And Alpha-Msh4-10 Cyclic Lactam Fragment Analogues Of Alpha-Melanotropin. The Cyclic Peptides Have The Following General Structures: Ac-[nle4,Xxx5,D-Phe7,Yyy10,Gly11]-Alpha-Msh4-13-Nh2 And Ac-[nle4,Xxx5,D-Phe7,Yyy10]-Alpha-Msh4-10-Nh2,Where Xxx = Glu Or Asp And Yyy = Lys,Orn,Dab,Or Dpr. Formation Of The Lactam Bridge Between The Side-Chain Groups Xxx And Yyy Was Performed Either In Solution Or On A Solid-Phase Support. Seven Cyclic Peptides Were Prepared And Bioassayed For Their Melanotropic Potency By Using Standard Frog (Rana Pipiens) And Lizard (Anolis Carolinensis) Skin Bioassays. Relative To Alpha-Msh (Relative Potency = 1),The Potencies Of The Cyclic Peptides In The Lizard Skin Bioassay Were As Follows: Alpha-Msh (1); Ac-[nle4,Glu5,D-Phe7,Lys10,Gly11]-Alpha-Msh4-13-Nh2 (6); Ac-[nle4,Asp5,D-Phe7,Lys10,Gly11]-Alpha-Msh4-13-Nh2 (100); Ac-[nle4,Glu5,D-Phe7,Lys10]-Alpha-Msh4-10-Nh2 (9); Ac-[nle4,Asp5,D-Phe7,Lys10]-Alpha-Msh4-10-Nh2 (90); Ac-[nle4,Asp5,D-Phe7,Orn10]-Alpha-Msh4-10-Nh2 (20); Ac-[nle4,Asp5,D-Phe7,Dab10]-Alpha-Msh4-10-Nh2 (5); Ac-[nle4,Asp5,D-Phe7,Dpr10]-Alpha-Msh4-10-Nh2 (5). Similar Results Were Obtained In The Frog Skin Bioassay,But The Analogues Were Much Less Potent. Cyclic Melanotropins With 23-Membered Rings Exhibited 100-Fold Higher Melanotropic Potency Than Alpha-Msh With Selectivity For The Lizard Melanocyte Receptors Over The Frog Melanocyte Receptors. Increasing Or Decreasing The Ring Size Of These Cyclic Melanotropins From 23 Diminishes The Biological Potency Of The Resulting Cyclic Peptide. The 23-And 24-Membered Ring Analogues Showed Prolonged (Residual) Biological Activities In Both Biological Assays,But The Smaller Ring Systems (20,21,22) Did Not. These Results Provide New Insights Into The Structural And Conformational Requirements Of Alpha-Msh And Its Analogues At Two Different Types Of Pigment Cell (Melanocyte) Receptors.
Doi:10.1021/jm00132A010

专利信息

专利号:WO-2024182268-A1
优先权日:2023-02-27
标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics
发明人：HAN AMY
权利人:REGENERON PHARMA
摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.

专利号:US-2006165683-A1
优先权日:2001-12-05
标题:Methods and compositions for control of bone formation via modulation of sympathetic tone
发明人：KARSENTY GERARD; TAKEDA SHU; ELEFTERIOU FLORENT
权利人:KARSENTY GERARD; TAKEDA SHU; ELEFTERIOU FLORENT
摘要:This invention relates to methods for treatment, diagnosis and prevention of bone disease and comprises methods including measurement and modulation of sympathetic tone and leptin activity. Alteration of sympathetic tone in bone disease can be accomplished by decreasing or increasing leptin synthesis, leptin receptor synthesis, leptin binding to the leptin receptor, and leptin receptor activity. Alteration of sympathetic tone in bone disease can also be accomplished in the foregoing manner, in combination with traditional sympathetic nervous system agonists and/or antagonists, such as, but not limited to, a dopamine β hydroxylase antagonist or a β adrenergic antagonist for treatment or prevention of osteoporosis.

专利号:US-2009325858-A1
优先权日:2003-03-21
标 题:Reduction of Zinc-Induced Neurotoxic Injury By Blockade of Nitric Oxide Synthesis
发明人：FREDERICKSON CHRISTOPHER J
权利人:ANDRO DIAGNOSTICS INC
摘要:The present invention provides methods of inhibiting release of zinc from neurons and of preventing zinc-mediated brain injury. Also provided are methods of improving cerebral blood flow while preventing zinc-mediated brain injury. Inhibitors of or activators of nitric oxide synthases modulate nitric oxide synthesis to reduce nitric oxide-induced release of neurotoxic amounts of zinc, thereby reducing zinc-mediated neuronal injury after brain trauma.

专利号:WO-2010129520-A1
优先权日:2009-05-06
标题 :Solid support for fmoc-solid phase synthesis of peptide acids

专利号:EP-2427474-A1
优先权日:2009-05-06
标题:Solid support for fmoc-solid phase synthesis of peptide acids

专利号:CA-2761265-C
优先权日:2009-05-06
标 题:Solid support for fmoc-solid phase synthesis of peptide acids