GlpBio

10Panx (trifluoroacetate salt)

目录号: GC52423纯度: >98.00%同义词: 10Panx1, WRQAAFVDSY
10Panx (trifluoroacetate salt)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。
10Panx (trifluoroacetate salt)
规格价格库存数量操作
1 mg¥448.00现货
1
5 mg¥1,232.00现货
1
10 mg¥2,240.00现货
1
25 mg¥5,026.00现货
1
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产品描述 Description

10Panx (trifluoroacetate salt) is a potent Panx1 channel inhibitor that targets the W74 to Y83 segment of the ECL1 of Panx1 protein [1]. 10Panx (trifluoroacetate salt) inhibits the P2X7 receptor activation-induced cleavage of caspase-1 and the processing and release of IL-1β by suppressing Panx1[2]. 10Panx (trifluoroacetate salt) has been widely used to alleviate the characteristic inflammatory responses in mouse models of asthma[3].

In vitro, 10Panx (trifluoroacetate salt) (50μM) treatment for 20 hours significantly inhibited the formation of capillary-like structures in human dermal lymphatic endothelial cells (HDLECs)[4]. Treatment with 10Panx (trifluoroacetate salt) 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 (trifluoroacetate salt) significantly inhibited cell proliferation[6].

In vivo, 10Panx (trifluoroacetate salt) 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 (trifluoroacetate salt) 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 (trifluoroacetate salt)) 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 (trifluoroacetate salt)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 (trifluoroacetate salt) 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 (trifluoroacetate salt)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 (trifluoroacetate salt)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 (trifluoroacetate salt)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 (trifluoroacetate salt)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 (trifluoroacetate salt)，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 (trifluoroacetate salt)，可降低大鼠第一磨牙诱导的牙本质敏感[8]。

实验参考方法 Experimental Reference Method

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 (trifluoroacetate salt) or PBS (vehicle) for 24, 48 and 72h. Cell viability was evaluated.

Reaction Conditions

200µM; 24, 48 and 72h

Applications

10Panx (trifluoroacetate salt) 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 (trifluoroacetate salt): (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 (trifluoroacetate salt) group, rats were administered intracerebroventricular injections of 10Panx (trifluoroacetate salt) (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 (trifluoroacetate salt) treatment significantly reduced the infarct volume and alleviate neurological deficits in MCAO model of rats.

References:
[1] 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.
[2] Wei R, Bao W, He F, et al. Pannexin1 channel inhibitor (10Panx (trifluoroacetate salt)) protects against transient focal cerebral ischemic injury by inhibiting RIP3 expression and inflammatory response in rats[J]. Neuroscience, 2020, 437: 23-33.

产品文档 Product Documents

Purity:>98.00%

化学性质Chemical Properties

同义词
10Panx1, WRQAAFVDSY
SMILES
OC(C=C1)=CC=C1C[C@@H](C(O)=O)NC([C@H](CO)NC([C@H](CC(O)=O)NC([C@H](C(C)C)NC([C@H](CC2=CC=CC=C2)NC([C@H](C)NC([C@H](C)NC([C@H](CCC(N)=O)NC([C@H](CCCNC(N)=N)NC([C@@H](N)CC3=CNC4=CC=CC=C34)=O)=O)=O)=O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O
分子式
C58H79N15O16 • XCF3COOH
分子量
1242.3 g/mol
溶解性
DMF: 5 mg/ml,DMSO: 2 mg/ml,PBS (pH 7.2): 1 mg/ml
保存条件
-20°C
General tips
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°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol