PCI-27483
(Synonyms: (S)-2-[[2-[5-(5-甲脒基-1H-苯并咪唑-2-基)-6,2'-二羟基-5'-氨基磺酰基联苯-3-基]乙酰基]氨基]琥珀酸) 目录号 : GC19277
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PCI-27483是一种可逆的小分子活化因子VIIa（FVIIa）抑制剂。
Cas No.:871266-63-6
Sample solution is provided at 25 µL, 10mM.
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PCI-27483 is a reversible small-molecule activated factor VIIa (FVIIa) inhibitor[1-2]. PCI-27483 selectively inhibits the FVIIa/tissue factor (TF) complex, blocking PAR-2 activation and its downstream signaling pathways. PCI-27483 can be used in research related to cancer therapy, antiviral and antithrombotic applications[3-4].
In vitro, pretreatment of human Calu-3 2B4 airway epithelial cells with PCI-27483 (100μM) for 1 hour, followed by infection with pseudovirions bearing the SARS-CoV-2 spike glycoprotein, moderately inhibited pseudovirus entry[5]. PCI-27483 (4μM) was combined with an anti-VEGFA antibody to treat tumor-derived human umbilical vein endothelial cells for 4-48 hour. The combination significantly inhibited cell proliferation, migration, and tube-forming capability, while also reducing CPT1A protein levels in the tumor-derived human umbilical vein endothelial cells[6].
References:
[1] Gómez-Outes A, Suárez-Gea ML, Lecumberri R, et al. New parenteral anticoagulants in development. Ther Adv Cardiovasc Dis. 2011 Feb;5(1):33-59.
[2] Ramanathan RK, Thomas GW, Khorana AA, et al. A Phase 2 Study of PCI-27483, a Factor VIIa Inhibitor in Combination with Gemcitabine for Advanced Pancreatic Cancer. Oncology. 2019;96(4):217-222.
[3] Bonardi A, Supuran CT. Polypharmacology of carbonic anhydrase inhibitors and activators. Expert Opin Pharmacother. 2025 Apr;26(5):567-580.
[4] Shrimp JH, Janiszewski J, Chen CZ, et al. Suite of TMPRSS2 Assays for Screening Drug Repurposing Candidates as Potential Treatments of COVID-19.
[5] Sun YJ, Velez G, Parsons DE, et al. Structure-based phylogeny identifies avoralstat as a TMPRSS2 inhibitor that prevents SARS-CoV-2 infection in mice. J Clin Invest. 2021 May 17;131(10):e147973.
[6] Huang N, Ren J, Deng X, et al. PIEZO1 as a new target for hyperglycemic stress-induced neuropathic injury: The potential therapeutic role of bezafibrate. Biomed Pharmacother. 2024 Jul;176:116837.
PCI-27483是一种可逆的小分子活化因子VIIa（FVIIa）抑制剂[1-2]。PCI-27483选择性抑制FVIIa/组织因子（TF）复合物，阻断PAR-2激活及下游信号通路。PCI-27483可用于肿瘤治疗、抗病毒、抗血栓的相关研究[3-4]。
在体外，PCI-27483（100μM）预处理人Calu-3 2B4气道上皮细胞1小时，随后用带有SARS-CoV-2刺突糖蛋白的假病毒感染，可适度抑制假病毒的进入[5]。PCI-27483（4μM）与抗VEGFA抗体联合处理肿瘤人脐静脉内皮细胞4-48小时。PCI-27483可显著抑制细胞的增殖、迁移和成管能力，同时在肿瘤人脐静脉内皮细胞中降低CPT1A蛋白水平[6]。
| Cell experiment [1]: | |
Cell lines | Calu-3 2B4 cells (human airway epithelial cell line) |
Preparation Method | Calu-3 2B4 cells were incubated with PCI-27483 (100μM) for 1 hour at 37°C. The cells were then transduced with VSV-based pseudovirions bearing the SARS-CoV-2 spike glycoprotein and a luciferase reporter, maintaining the same concentration of compounds, and incubated overnight. |
Reaction Conditions | 100μM; 1h pretreatment followed by pseudovirus infection. |
Applications | PCI-27483 displayed modest inhibition of SARS-CoV-2 pseudovirus entry into Calu-3 2B4 cells. |
References: | |
| Cas No. | 871266-63-6 | SDF | |
| 别名 | (S)-2-[[2-[5-(5-甲脒基-1H-苯并咪唑-2-基)-6,2'-二羟基-5'-氨基磺酰基联苯-3-基]乙酰基]氨基]琥珀酸 | ||
| Canonical SMILES | O=C(O)C[C@@H](C(O)=O)NC(CC1=CC(C2=CC(S(=O)(N)=O)=CC=C2O)=C(O)C(C3=NC4=CC=C(C(N)=N)C=C4N3)=C1)=O | ||
| 分子式 | C26H24N6O9S | 分子量 | 596.57 |
| 溶解度 | DMSO : 62.5 mg/mL (104.77 mM) | 储存条件 | Store at -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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6762 mL | 8.3812 mL | 16.7625 mL |
| 5 mM | 335.2 μL | 1.6762 mL | 3.3525 mL |
| 10 mM | 167.6 μL | 838.1 μL | 1.6762 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet