|(R)-2-((S)-2-苯甲酰胺-3-(1H-吲哚-3-基)丙酰胺基)-3-苯基丙酸甲酯|CsnPharm

CAS No.: 1435265-06-7

HCH6-1 Catalog No. CSN25309

Synonyms: HCH6-1

HCH6-1 is a competitive antagonist of Formyl peptide receptor 1 (FPR1) and may have potential as a new therapeutic agent for treating FPR1-involved inflammatory lung diseases.

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生物活性

实验方案

技术信息

生物活性

描述During the inflammatory process, neutrophils are recruited into inflammatory areas to eliminate invasive pathogens. Formyl peptide receptor 1 (FPR1) typically facilitates neutrophil immune responses in the presence of N-formyl peptides derived from bacteria in vitro. HCH6-1, a competitive dipeptide antagonist of FPR1, shows a potent inhibitory eﬀect on FPR1-agonist-activated human neutrophils. HCH6-1 signiﬁcantly inhibited superoxide anion generation in fMLF (FPR1 agonist)-activated neutrophils, with IC₅₀ of 0.32 ± 0.03 μM. Further, HCH6-1 signiﬁcantly inhibited elastase release in fMLF-activated neutrophils, with IC₅₀ of 0.57 ± 0.07 μM. HCH6-1 dose dependently diminished CD11b expression up-regulated by fMLF in human neutrophils. Furthermore, HCH6-1 reduced the neutrophil migration induced by fMLF suggesting that HCH6-1 impaired chemotaxis only in FPR1-activated neutrophils. Compared with the controls, in treated neutrophils, HCH6-1 dose-dependently inhibited the binding of FNLFNYK to FPR1. The protective eﬀect of HCH6-1 in LPS (lipopolysaccharide)-induced ALI (acute lung injury) was tested in vivo. HCH6-1 pretreatment reduced inﬂammatory cell inﬁltration and distortion of pulmonary architecture in the presence of LPS^[1].
参考文献

[1] Yang SC, Chang SH, Hsieh PW, et al. Dipeptide HCH6-1 inhibits neutrophil activation and protects against acute lung injury by blocking FPR1. Free Radic Biol Med. 2017;106:254-269

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
- 2.1298 mL
- 10.6489 mL
- 21.2978 mL
- 5 mM
- 0.4260 mL
- 2.1298 mL
- 4.2596 mL
- 10 mM
- 0.2130 mL
- 1.0649 mL
- 2.1298 mL

技术信息

CAS号

1435265-06-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H27N3O4

运输

蓝冰

分子量

469.53

别名

HCH6-1

溶解度

DMSO	94.0 mg/mL (200.2 mM)
Water	Insoluble
Ethanol	8.0 mg/mL (17.0 mM)

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