10Panx是一种强效的Panx1通道抑制剂，靶向Panx1蛋白ECL1结构域中的W74至Y83片段。
Cas No.:955091-53-9
Sample solution is provided at 25 µL, 10mM.
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10Panx is a potent Panx1 channel inhibitor that targets the W74 to Y83 segment of the ECL1 of Panx1 protein [1]. 10Panx inhibits the P2X7 receptor activation-induced cleavage of caspase-1 and the processing and release of IL-1β by suppressing Panx1[2]. 10Panx has been widely used to alleviate the characteristic inflammatory responses in mouse models of asthma[3].
In vitro, 10Panx (50μM) treatment for 20 hours significantly inhibited the formation of capillary-like structures in human dermal lymphatic endothelial cells (HDLECs)[4]. Treatment with 10Panx at a concentration of 100μM for 6 hours delays the maturation of bovine oocytes and reduces the level of reactive oxygen species within the cells[5]. The 72h treatment of HCT116 cells with 200μM 10Panx significantly inhibited cell proliferation[6].
In vivo, 10Panx treatment via intraventricular injection of 5μl (2μg/μl) 0.5 hours before middle cerebral artery occlusion (MCAO) can reduce the infarct volume in rats and alleviate neurological deficits[7]. A single intravenous injection of 2.58nmol/g dose of 10Panx reduced the induced dentin hypersensitivity of the first molar in rats[8].
References:
[1] Jiang M, Li X, Xie K. Pannexin channels in inflammation and tumorigenesis[J]. Frontiers in Cell and Developmental Biology, 2025, 13: 1647765.
[2] Pelegrin P, Surprenant A. Pannexin‐1 mediates large pore formation and interleukin‐1β release by the ATP‐gated P2X7 receptor[J]. The EMBO journal, 2006, 25(21): 5071-5082.
[3] Martinez L A, Rasky A J, Morris S B, et al. Inhibition of Pannexin1 hemichannels in the airways epithelium reduces the characteristic inflammatory response in an asthmatic mouse model[J]. World Allergy Organization Journal, 2020, 13(8).
[4] Boucher J, Simonneau C, Denet G, et al. Pannexin-1 in human lymphatic endothelial cells regulates lymphangiogenesis[J]. International Journal of Molecular Sciences, 2018, 19(6): 1558.
[5] Dye Z T, Rutledge L V, Penuela S, et al. Pannexin 1 inhibition delays maturation and improves development of Bos taurus oocytes[J]. Journal of Ovarian Research, 2020, 13(1): 98.
[6] Fierro-Arenas A, Landskron G, Camhi-Vainroj I, et al. Pannexin-1 expression in tumor cells correlates with colon cancer progression and survival[J]. Life Sciences, 2024, 351: 122851.
[7] Wei R, Bao W, He F, et al. Pannexin1 channel inhibitor (10panx) protects against transient focal cerebral ischemic injury by inhibiting RIP3 expression and inflammatory response in rats[J]. Neuroscience, 2020, 437: 23-33.
[8] Ohyama S, Ouchi T, Kimura M, et al. Piezo1-pannexin-1-P2X3 axis in odontoblasts and neurons mediates sensory transduction in dentinal sensitivity[J]. Frontiers in physiology, 2022, 13: 891759.
10Panx是一种强效的Panx1通道抑制剂，靶向Panx1蛋白ECL1结构域中的W74至Y83片段[1]。10Panx 通过抑制Panx1来阻止P2X7受体激活诱导的caspase-1裂解以及IL-1β的加工和释放[2]。10Panx已被广泛用于减轻哮喘小鼠模型中的特征性炎症反应[3]。
在体外，50μM的10Panx处理人真皮淋巴内皮细胞(HDLECs)20小时，显著抑制了毛细管样结构的形成[4]。100μM的10Panx处理牛卵母细胞6小时，会延迟卵母细胞的成熟并降低细胞内的活性氧水平[5]。200μM的10Panx处理HCT116细胞72小时，显著抑制了细胞增殖[6]。
在体内，在大脑中动脉闭塞（MCAO）前0.5小时，脑室内注射5µl（2µg/µl）10Panx，可减少大鼠的梗死体积并减轻神经功能缺损[7]。单次静脉注射2.58nmol/g剂量的 10Panx，可降低大鼠第一磨牙诱导的牙本质敏感[8]。
| Cell experiment [1]: | |
Cell lines | HCT116 cells |
Preparation Method | HCT116 cells were grown in DMEM medium with 10% (v/v) fetal bovine serum (FBS), 100μg/ml streptomycin, and 100U/ml penicillin at 37°C in 5% CO2/atmosphere. HCT116 cells were seeded in triplicates at a density of 1×104 cells per well in the 96-well plates containing 100μl culture medium (1% FBS) and allowed to adhere in a 5% CO2 incubator at 37°C overnight. Cells were treated with 200μM 10Panx or PBS (vehicle) for 24, 48 and 72h. Cell viability was evaluated. |
Reaction Conditions | 200µM; 24, 48 and 72h |
Applications | 10Panx treatment significantly reduced the cell viability of HCT116 cells in a time-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male Sprague-Dawley rats |
Preparation Method | Male Sprague-Dawley rats (250-280g) were housed singly in a standard environment with food and water ad libitum. A total of 80 rats were randomly assigned to 3 groups and treated with or without 10Panx: (1) in the sham group (n = 14), rats received anesthesia and vehicle injection; (2) in the surgery plus vehicle group, rats underwent MCAO under isoflurane anesthesia, and vehicle was administered intracerebroventricularly 30min before ischemia onset (n = 22) ; and (3) in the surgery plus 10Panx group, rats were administered intracerebroventricular injections of 10Panx (2μg/μl; 5μl) at 0.5h before MCAO under isoflurane anesthesia. Rats were sacrificed 48 hours after MCAO for experiments and the brain tissues were collected for analysis. |
Dosage form | 2μg/μl (5μl) for once; i.c.v. |
Applications | 10Panx treatment significantly reduced the infarct volume and alleviate neurological deficits in MCAO model of rats. |
References: | |
| Cas No. | 955091-53-9 | SDF | |
| 别名 | 10Panx | ||
| Canonical SMILES | CC(C)C(C(=O)NC(CC(=O)O)C(=O)NC(CO)C(=O)NC(CC1=CC=C(C=C1)O)C(=O)O)NC(=O)C(CC2=CC=CC=C2)NC(=O)C(C)NC(=O)C(C)NC(=O)C(CCC(=O)N)NC(=O)C(CCCN=C(N)N)NC(=O)C(CC3=CNC4=CC=CC=C43)N | ||
| 分子式 | C58H79N15O16 | 分子量 | 1242.37 |
| 溶解度 | ≥ 124.2mg/mL in DMSO | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg |
| 1 mM | 804.9 μL | 4.0246 mL | 8.0491 mL |
| 5 mM | 161 μL | 804.9 μL | 1.6098 mL |
| 10 mM | 80.5 μL | 402.5 μL | 804.9 μL |
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