[D-Lys3]-GHRP-6
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50:0.9 μM
[D-Lys3] -GHRP-6是一种ghrelin受体(GHS-R1a)拮抗剂,微弱结合黑皮质素受体(Ki = 26-120 μM)。
体外:[D-Lysa]GHRP-6使用类似的亲和力结合所有四个MC受体,而不与结构上相关的Met-脑啡肽和功能相关的GHuRH,以及LHRH和促生长素抑制素14结合。这(GH释放/脑啡肽的低亲和力)可表明其在药理学浓度下不与MC受体相互作用。[DLys3] GHRP-6仅用比GHRP-6略微更高的亲和力结合到MC1受体。 [1]。
与GHRP-6相比,[D-Lys3] GHRP-6对所有MC受体,特别是对MC3和MC4受体具有更高的亲和力。有趣的是,[D-Lys 3] GHRP-6仅用比GHRP-6略微更高的亲和力结合MC1受体,这可表明在位点8的碱性亲水残基对MC 1受体(与其他MC受体亚型相同)不重要 [1,2]。肽类GHS受体拮抗剂(D-Lys3)-GHRP-6(10-4 M)微弱拮抗ghrelin (10-7 M),对GHS-受体(IC50,0.9×10 -6 M)呈现出比ghrelin(IC50,0.3×10 -9 M)弱得多的亲和力。Ghrelin增加76%的被瘦素(n=17)抑制的细胞中的电活动性。这些数据表明,ghrelin与弓状核中瘦素下丘脑网络相互作用。瘦素和ghrelin在弓状核神经元中起相反作用,可作为它们促进食欲和抑制食欲作用的神经生理学相关成分[2]。
体内:单独给药D-Lys3-GHRP-6(一种GHS受体拮抗剂)对GH分泌无显著影响。相反,用该拮抗剂预处理有效地抑制AMPA和NMDA对GH分泌的刺激作用。为证实这一争论,实施进一步实验以评估D-Lys3-GHRP-6给药的不同方案(剂量、时间、额外的GHS受体拮抗剂)。然而,ghrelin可能仅介入GH分泌不足或GH分泌过多的情况,但不参与基础GH分泌的控制[2]。
临床试验:目前尚未进行临床研究。
参考文献:
[1]. Schith HB, Muceniece R, Wikberg JE. Characterization of the binding of MSH-B, HB-228, GHRP-6 and 153N-6 to the human melanocortin receptor subtypes. Neuropeptides. 1997 Dec;31(6):565-71.
[2]. Traebert M, Riediger T, Whitebread S, Scharrer E, Schmid HA. Ghrelin acts on leptin-responsive neurones in the rat arcuate nucleus. J Neuroendocrinol. 2002 Jul;14(7):580-6.
[3]. Pinilla L, Barreiro ML, Tena-Sempere M, Aguilar E.Role of ghrelin in the control of growth hormone secretion in prepubertal rats: interactions with excitatory amino acids. Neuroendocrinology. 2003 Feb;77(2):83-90.
- 1. Caishun Zhang, Junhua Yuan, et al. "Ghrelin in the lateral parabrachial nucleus influences the excitability of glucosensing neurons, increases food intake and body weight." Endocr Connect. 2020 Oct 1;EC-20-0285.R1. PMID:33112816
- 2. Fan XT, Tian Z, et al. "Ghrelin Receptor Is Required for the Effect of Nesfatin-1 on Glucose Metabolism." Front Endocrinol (Lausanne). 2018 Oct 24;9:633. PMID:30405536
Physical Appearance | White lyophilised solid |
Storage | Desiccate at -20°C |
M.Wt | 930.12 |
Cas No. | 136054-22-3 |
Formula | C49H63N13O6 |
Solubility | ≥51.1 mg/mL in DMSO; ≥51.8 mg/mL in EtOH; ≥50.7 mg/mL in H2O |
SDF | Download SDF |
Canonical SMILES | NCCCC[C@@](/N=C(O)/[C@@](/N=C(O)/[C@](/N=C(O)/[C@@](/N=C(O)/[C@@](/N=C(O)/[C@](N)([H])CC1=CN=CN1)([H])CC2=CNC3=CC=CC=C23)([H])CCCCN)([H])CC4=CNC5=CC=CC=C45)([H])CC6=CC=CC=C6)([H])C(O)=N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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