HCH6-1
目录号: PL01208 纯度: ≥99%
CAS No. :1435265-06-7
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中文名称
HCH6-1
英文名称
HCH6-1
英文别名
HCH6-1;N-Benzoyl-L-Trp-D-Phe-OMe;Methyl benzoyl-L-tryptophyl-D-phenylalaninate;Methyl (2R)-2-[[(2S)-2-benzamido-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoate
Cas No.
1435265-06-7
分子式
C28H27N3O4
分子量
469.53
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
HCH6-1 是一种有效的甲酰肽受体 1 (FPR1) 的竞争性二肽拮抗剂。HCH6-1 抑制 fMLF (FPR1激动剂) 特异性激活的人中性粒细胞的趋化性、超氧阴离子生成和弹性酶释放。动物实验中,HCH6-1 对急性肺损伤 (ALI) 具有保护作用,可用于 FPR1 参与的炎症性肺部疾病的研究。
生物活性
HCH6-1 is a potent and competitive dipeptide antagonist of Formyl peptide receptor 1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, and elastase release in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI) in vivo and can be used for the research of FPR1-involved inflammatory lung diseases.
性状
Solid
IC50 & Target[1][2]
IC50: Formyl peptide receptor 1 (FPR1)
体外研究(In Vitro)
In a cell-impermeable cytochrome c reduction assay, HCH6-1 significantly inhibits superoxide anion generation in fMLF (FPR1 agonist)-activated neutrophils with an IC50 of 0.32 μM. HCH6-1 has fewer inhibitory effects in WKYMVm (dual FPR1/FPR2 agonist)- and MMK1 (FPR2 agonist)-activated neutrophils, with IC50s of 4.98±0.27 μM and 17.68±2.77 μM, respectively.
HCH6-1 does not induce LDH release even at 30 μM, so it does not have cytotoxic effects in human neutrophils. HCH6-1 does not alter the level of xanthine/xanthine oxidase superoxide anion and DPPH radical in cell-free systems.
HCH6-1 significantly inhibits elastase release in fMLF-activated neutrophils, with an IC50 of 0.57 μM. However, in neutrophils triggered by WKYMVm or MMK1, HCH6-1 inhibits elastase release at higher concentrations, with IC50s of 5.22±0.69 μM and
体内研究(In Vivo)
HCH6-1 (intraperitoneal injection; 50 mg/kg; 1 h before LPS spray or 30 min after LPS spray) alone does not induce airspace inflammation. HCH6-1 pretreatment reduces inflammatory cell infiltration and distortion of pulmonary architecture in the presence of LPS. HCH6-1 posttreatment shows inhibitory effects on neutrophil accumulation and lung damage in LPS-induced ALI mice.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Yang SC, et al. Dipeptide HCH6-1 inhibits neutrophil activation and protects against acute lung injury by blocking FPR1. Free Radic Biol Med. 2017 May;106:254-269
溶解度数据
In Vitro: DMSO : 250 mg/mL (532.45 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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