|N-((S)-1-(((2S,3S)-1-((6-氨基-6-氧代己基)氨基)-3-甲基-1-氧代戊烷-2-基)氨基)-3-(4-羟基苯基)-1-氧代丙烷-2-基)己酰胺醋酸盐|CsnPharm

CAS No.: 2453297-24-8

N-((S)-1-(((2S,3S)-1-((6-Amino-6-oxohexyl)amino)-3-methyl-1-oxopentan-2-yl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)hexanamide acetate Catalog No. CSN24316

Dihexa is a blood-brain barrier-permeable angiotensin IV analog which exhibits high affinity to HGF with Kd value of 65pM and induces c-Met phosphorylation in the presence of subthreshold concentrations of HGF and augment HGF-dependent cell scattering.

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技术信息

生物活性

描述Dihexa (acetate), an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa binds with high affinity to HGF and both dihexa and its parent compound Norleucine 1-AngIV induce c-Met phosphorylation in the presence of subthreshold concentrations of HGF and augment HGF-dependent cell scattering. Dihexa effectively inhibits HGF dimerization at 1 μM. While dihexa at 1 nM and 10 pM alone does not activate c-Met, it markedly augments the capacity of HGF at 1.25 and 2.5 ng/mL to activate c-Met^[1]. Dihexa exhibits procognitive activity may have therapeutic potential as a treatment of Alzheimer's disease. Dihexa reverses scopolamine-dependent spatial learning deficits. It improves spatial learning in aged rats. Dihexa induces spinogenesis in cultured hippocampal neurons^[2]. A Dihexa concentration of 1 μM confers optimal protection from acute treatment with either ototoxin. Pretreatment with Dihexa does not affect the amount of fluorescently tagged gentamicin that enters hair cells, indicating that Dihexa's protection is likely mediated by intracellular events and not by inhibiting aminoglycoside entry^[3].
参考文献

[1] Benoist CC, Kawas LH, Zhu M, Tyson KA, Stillmaker L, Appleyard SM, Wright JW, Wayman GA, Harding JW. The procognitive and synaptogenic effects of angiotensin IV-derived peptides are dependent on activation of the hepatocyte growth factor/c-met system. J Pharmacol Exp Ther. 2014 Nov;351(2):390-402. doi: 10.1124/jpet.114.218735. Epub 2014 Sep 3
[2] McCoy AT, Benoist CC, Wright JW, Kawas LH, Bule-Ghogare JM, Zhu M, Appleyard SM, Wayman GA, Harding JW. Evaluation of metabolically stabilized angiotensin IV analogs as procognitive/antidementia agents. J Pharmacol Exp Ther. 2013 Jan;344(1):141-54
[3] Uribe PM, Kawas LH, Harding JW, Coffin AB. Hepatocyte growth factor mimetic protects lateral line hair cells from aminoglycoside exposure. Front Cell Neurosci. 2015 Jan 28;9:3

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.7708 mL
- 8.8540 mL
- 17.7081 mL
- 5 mM
- 0.3542 mL
- 1.7708 mL
- 3.5416 mL
- 10 mM
- 0.1771 mL
- 0.8854 mL
- 1.7708 mL

技术信息

CAS号	2453297-24-8	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C29H48N4O7	运输	蓝冰
分子量	564.71	别名

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N-((S)-1-(((2S,3S)-1-((6-Amino-6-oxohexyl)amino)-3-methyl-1-oxopentan-2-yl)amino)-3-(4-hydroxyphenyl)-1-oxopropan-2-yl)hexanamide acetate Catalog No. CSN24316

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