Antileukinate是一种强效的α-chemokine受体结合抑制剂，可抑制Growth-related oncogene-α (GROα)与相关受体的结合。
Cas No.:138559-60-1
Sample solution is provided at 25 µL, 10mM.
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Antileukinate is a potent inhibitor of α-chemokine receptor binding, which inhibits the binding of Growth-related oncogene-α (GROα) to the related receptors [1]. Antileukinate inhibited the binding of 125I-labeled eotaxin to eosinophils with an IC50 value of 8.2μM[2]. Antileukinate binds to CXC receptors 1 and 2 on neutrophils, thereby inhibiting IL-8-induced neutrophil chemotaxis and degranulation [3]. Antileukinate has been widely used to reduce the levels of oxidative stress markers in mouse models with lung injury and to improve lung function[4].
In vitro, Antileukinate treatment (100μM) for 24 hours significantly inhibited the proliferation of human umbilical vein endothelial cells (HUVECs) and the binding of GROα[5]. Treatment with 200μM Antileukinate for 24 hours significantly inhibited the growth of HT-29 cells and promoted cell lysis[6].
In vivo, Antileukinate treatment via a single subcutaneous dose (0.4mg) for 24 hours significantly suppressed hemorrhage-induced priming for acute lung injury in mice [7]. Thirty minutes before injecting caerulein into mice, a single dose of Antileukinate (52.63mg/kg) was subcutaneously administered, which significantly reduced the severity of acute pancreatitis induced by caerulein, alleviated acinar cell damage and edema[8].
References:
[1] Fujisawa N, Hayashi S, Miller E J. A synthetic peptide inhibitor for α-chemokines inhibits the tumour growth and pulmonary metastasis of human melanoma cells in nude mice[J]. Melanoma Research, 1999, 9(2): 105-114.
[2] Fukuno Y, Hayashi S, Kohsa K, et al. Chemokine receptor inhibitor, Antileukinate, suppressed ovalbumin-induced eosinophilic inflammation in the airway[J]. Cytokine, 2003, 22(5): 116-125.
[3] Kamity R, Patel H, Younis S, et al. Inhibition of CXCR 1 and 2 delays preterm delivery and reduces neonatal mortality in a mouse model of chorioamnionitis[J]. European Journal of Inflammation, 2014, 12(3): 447-457.
[4] Poggi C, Dani C. Antioxidant strategies and respiratory disease of the preterm newborn: an update[J]. Oxidative medicine and cellular longevity, 2014, 2014(1): 721043.
[5] Fujisawa N, Hayashi S, Kurdowska A, et al. Inhibition of GROα-induced human endothelial cell proliferation by the α-chemokine inhibitor antileukinate[J]. Cytokine, 1999, 11(3): 231-238.
[6] Fujisawa N, Sakao Y, Hayashi S, et al. α-Chemokine growth factors for adenocarcinomas; a synthetic peptide inhibitor for α-chemokines inhibits the growth of adenocarcinoma cell lines[J]. Journal of cancer research and clinical oncology, 2000, 126(1): 19-26.
[7] Lomas-Neira J L, Chung C S, Grutkoski P S, et al. CXCR2 inhibition suppresses hemorrhage-induced priming for acute lung injury in mice[J]. Journal of leukocyte biology, 2004, 76(1): 58-64.
[8] Bhatia M, Hegde A. Treatment with antileukinate, a CXCR2 chemokine receptor antagonist, protects mice against acute pancreatitis and associated lung injury[J]. Regulatory peptides, 2007, 138(1): 40-48.
Antileukinate是一种强效的α-chemokine受体结合抑制剂，可抑制Growth-related oncogene-α (GROα)与相关受体的结合[1]。Antileukinate抑制125I标记的嗜酸粒细胞趋化因子与嗜酸性粒细胞结合，IC50值为8.2μM[2]。Antileukinate与中性粒细胞上的CXC受体1和2结合，从而抑制IL-8诱导的中性粒细胞趋化和脱颗粒[3]。Antileukinate已被广泛用于降低肺损伤小鼠模型中氧化应激标志物的水平并改善肺功能[4]。
在体外，使用100μM的Antileukinate处理人脐静脉内皮细胞(HUVECs)24小时，显著抑制了细胞增殖和GROα的结合[5]。使用200μM的Antileukinate处理HT-29细胞24小时，显著抑制了细胞生长并促进了细胞裂解[6]。
在体内，单次皮下注射0.4mg剂量的Antileukinate处理24小时，显著抑制了小鼠出血引发的急性肺损伤易感性[7]。在向小鼠注射caerulein前30分钟，单次皮下注射52.63mg/kg剂量的Antileukinate，显著降低了caerulein诱导的急性胰腺炎的严重程度，减轻了腺泡细胞损伤和水肿[8]。
| Cell experiment [1]: | |
Cell lines | Human umbilical vein endothelial cells (HUVECs) |
Preparation Method | HUVECs were cultured in RPMI 1640 medium supplemented with 10% fetal bovine serum (FBS), 1% penicillin-streptomycin at 37℃ in the presence of 5% CO2. HUVECs were plated at a density of 5×104 cells/well in 96-well plate with growth medium for 4h, the medium was then aspirated and replaced with RPMI 1640 without FBS or ECGF and the cells were cultured for a further 16h. Serum-starved HUVEC were incubated with the different concentrations of Antileukinate (0, 20, 40, 60, 80, and 100µM) for 24h, then analyzed the cell viability. |
Reaction Conditions | 0, 20, 40, 60, 80, and 100µM; 24h |
Applications | Antileukinate treatment significantly reduced the cell viability of HUVECs in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Swiss mice |
Preparation Method | Swiss mice (20-25g) were housed in temperature (23±2°C) and light-controlled (12:12-hour light-dark cycle) animal care facility with food and tap water ad libitum. Mice were randomly assigned to control or experimental groups using eight or more animals for each group. Mice were given hourly intra-peritoneal (i.p.) injections of normal saline or caerulein (50μg/kg) in saline for 10h. Antileukinate or vehicle (PBS) was administered to caerulein-treated mice at a dose of 52.63mg/kg, s.c. 30min before (pre-treatment) the first caerulein injection. Collect pancreatic samples from mice for analysis. |
Dosage form | 52.63mg/kg for once; s.c. |
Applications | Antileukinate treatment alleviated acinar cell damage and edema induced by caerulein in mice. |
References: | |
| Cas No. | 138559-60-1 | SDF | |
| Canonical SMILES | CC(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC1=CNC2=C1C=CC=C2)C(N[C@@H](CC3=CNC4=C3C=CC=C4)C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N)=O)=O)CS)=O)=O)=O)=O)CCCNC(N)=N)=O | ||
| 分子式 | C45H66N18O7S | 分子量 | 1003.2 |
| 溶解度 | DMF: 1 mg/ml,DMSO: 5 mg/ml,PBS (pH 7.2): 2 mg/ml | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 996.8 μL | 4.9841 mL | 9.9681 mL |
| 5 mM | 199.4 μL | 996.8 μL | 1.9936 mL |
| 10 mM | 99.7 μL | 498.4 μL | 996.8 μL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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