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HCH6-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HCH6-1图片
CAS NO:1435265-06-7
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品介绍
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 ofFormyl peptide receptor1 (FPR1). HCH6-1 inhibits chemotaxis, superoxide anion generation, andelastaserelease in human neutrophils specifically activated by fMLF (an FPR1 agonist). HCH6-1 has protective effects against acute lung injury (ALI)in vivoand can be used for the research of FPR1-involved inflammatory lung diseases[1].

IC50& Target

IC50: Formyl peptide receptor 1 (FPR1)[1]

体外研究
(In Vitro)

In a cell-impermeable cytochromecreduction assay, HCH6-1 significantly inhibits superoxide anion generation in fMLF (FPR1 agonist)-activated neutrophils with an IC50of 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[1].
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[1].
HCH6-1 significantly inhibits elastase release in fMLF-activated neutrophils, with an IC50of 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 10.00±0.65 μM, respectively[1].

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[1].

Animal Model:C57BL/6 mice (20-25 g, 7-8 weeks old)[1]
Dosage:50 mg/kg
Administration:Intraperitoneal injection; 50 mg/kg; 1 h before LPS spray or 30 min after LPS spray
Result:Ameliorated ALI in LPS-induced mice.
HCH6-1-mediated decreasing of neutrophil recruitment serves as a protective mechanism in ALI mice.
分子量

469.53

性状

Solid

Formula

C28H27N3O4

CAS 号

1435265-06-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL(532.45 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1298 mL10.6489 mL21.2979 mL
5 mM0.4260 mL2.1298 mL4.2596 mL
10 mM0.2130 mL1.0649 mL2.1298 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.43 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (4.43 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.43 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。