Ceapin-A7
(Synonyms: N-(1-(2,4-双(三氟甲基)苄基)-1H-吡唑-4-基)-5-(呋喃-2-基)异恶唑-3-甲酰胺) 目录号 : GC61606
Ceapin-A7是一种内质网应激ATF6α信号的选择性阻断剂（IC50=0.59μM）。
Cas No.:2323027-38-7
Sample solution is provided at 25 µL, 10mM.
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Ceapin-A7 is a selective blocker of endoplasmic reticulum stress ATF6α signaling (IC50= 0.59μM)[1]. Ceapin-A7 can inhibit Th17 cell differentiation[2]. Ceapin-A7 protects cells from Zika virus infection and also has the function of increasing the radiosensitivity of cancer cells[3-4].
In vitro, pretreatment of ccRCC cells (ACHN and 786-O) with Ceapin-A7 (20μM) for 24 hours reduced the protein expression of PINK1 and BNIP3, and promoted cell proliferation and migration[5]. Pretreatment of bovine pulmonary artery endothelial cells (BPAEC) with Ceapin-A7 (15μM) for 24 hours, followed by stimulation with LPS (1μg/ml) for 2 hours, significantly enhanced the phosphorylation activation of STAT3, JAK2, and JNK, while exacerbating the inhibition of cell proliferation[6].
In vivo, Ceapin-A7 (10mg/kg) was administered via intraperitoneal injection three times per week to DBA/1J mice with collagen-induced arthritis (CIA), from day 22 to day 45, Ceapin-A7 significantly alleviated arthritis severity and joint bone erosion[7]. Ceapin-A7 (1μM) was administered via drinking water to curdlan-induced SKG mice, from week 1 until week 12. Ceapin-A7 significantly alleviated spinal ankylosis and osteophyte formation[8].
References:
[1] Fakir S, Sigdel M, Sarker MMR, et al. Ceapin-A7 suppresses the protective effects of Octreotide in human and bovine lung endothelial cells. Cell Stress Chaperones. 2025 Feb;30(1):1-8.
[2] Kubra KT, Akhter MS, Saini Y, et al. Activating transcription factor 6 protects against endothelial barrier dysfunction. Cell Signal. 2022 Nov;99:110432.
[3] Kern J, Schilling D, Schneeweis C, et al. Identification of the unfolded protein response pathway as target for radiosensitization in pancreatic cancer. Radiother Oncol. 2024 Feb;191:110059.
[4] Mufrrih M, Chen B, Chan SW. Zika Virus Induces an Atypical Tripartite Unfolded Protein Response with Sustained Sensor and Transient Effector Activation and a Blunted BiP Response. mSphere. 2021 Jun 30;6(3):e0036121.
[5] Yan M, Wang J, Wang H, et al. Knockdown of NR3C1 inhibits the proliferation and migration of clear cell renal cell carcinoma through activating endoplasmic reticulum stress-mitophagy. J Transl Med. 2023 Oct 8;21(1):701.
[6] Kubra KT, Barabutis N. Ceapin-A7 potentiates lipopolysaccharide-induced endothelial injury. J Biochem Mol Toxicol. 2023 Nov;37(11):e23460.
[7] Ge L, Wang T, Shi D, et al. ATF6α contributes to rheumatoid arthritis by inducing inflammatory cytokine production and apoptosis resistance. Front Immunol. 2022 Oct 10;13:965708.
[8] Ma M, Li H, Wang P, et al. ATF6 aggravates angiogenesis-osteogenesis coupling during ankylosing spondylitis by mediating FGF2 expression in chondrocytes. iScience. 2021 Jun 28;24(7):102791.
Ceapin-A7是一种内质网应激ATF6α信号的选择性阻断剂（IC50=0.59μM）[1]。Ceapin-A7能抑制Th17细胞分化[2]。Ceapin-A7保护细胞避免寨卡病毒的感染，还具备增加癌细胞放疗敏感性的功能[3-4]。
在体外，Ceapin-A7（20μM）预处理ccRCC细胞（ACHN和786-O）24小时，降低了PINK1和BNIP3的蛋白表达，促进细胞增殖和迁移[5]。Ceapin-A7（15μM）预处理牛肺动脉内皮细胞（BPAEC）24小时，随后以LPS（1μg/ml）刺激2小时，显著增强STAT3、JAK2和JNK的磷酸化激活，同时加剧细胞增殖抑制[6]。
在体内，Ceapin-A7（10mg/kg）每周三次腹腔注射，用于处理胶原诱导的关节炎（CIA）DBA/1J小鼠，从第22天至第45天，Ceapin-A7显著减轻了关节炎严重程度和关节骨侵蚀[7]。Ceapin-A7（1μM）通过饮水给药，用于处理经curdlan诱导的SKG小鼠，从第1周开始直至第12周。Ceapin-A7显著减轻了脊柱强直和骨赘形成[8]。
| Cell experiment [1]: | |
Cell lines | ACHN and 786-O cells (human renal cell carcinoma cell lines) |
Preparation Method | ACHN and 786-O cells were maintained in RPMI-1640 medium supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. Cells were treated with Ceapin-A7 at a concentration of 20μM for 5 hours. |
Reaction Conditions | 20μM; 5h |
Applications | Ceapin-A7 significantly down-regulated the expression of PINK1 and BNIP3 in NR3C1-knockdown ccRCC cells. Ceapin-A7 also reversed the increased LC3 expression and decreased P62 expression induced by NR3C1 knockdown, indicating inhibition of mitophagy. Additionally, Ceapin-A7 treatment rescued the reduced proliferation and migration capabilities of ccRCC cells caused by NR3C1 knockdown. |
| Animal experiment [2]: | |
Animal models | DBA/1J mice with collagen-induced arthritis (CIA) |
Preparation Method | CIA mice were intraperitoneally administered Ceapin-A7 (10mg/kg) three times per week from day 22 to day 45 post-immunization. Control groups received vehicle or etanercept (2mg/kg). |
Dosage form | 10mg/kg/day; i.p. |
Applications | Ceapin-A7 administration significantly reduced arthritis severity scores and paw swelling in CIA mice, comparable to etanercept treatment. Ceapin-A7 treatment decreased bone erosion parameters (Tb.Sp) while increasing bone mineral density (Tb.BMD) and trabecular number (Tb.N). Additionally, Ceapin-A7 reduced serum levels of inflammatory cytokines including IL-6, IL-8, TNF-α and IL-1β. Histological analysis showed Ceapin-A7 ameliorated synovial hyperplasia, pannus formation and cartilage destruction. |
References: | |
| Cas No. | 2323027-38-7 | SDF | |
| 别名 | N-(1-(2,4-双(三氟甲基)苄基)-1H-吡唑-4-基)-5-(呋喃-2-基)异恶唑-3-甲酰胺 | ||
| Canonical SMILES | O=C(NC1=CN(CC2=CC=C(C(F)(F)F)C=C2C(F)(F)F)N=C1)C3=NOC(C4=CC=CO4)=C3 | ||
| 分子式 | C20H12F6N4O3 | 分子量 | 470.32 |
| 溶解度 | DMSO: 100 mg/mL (212.62 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 | 2.1262 mL | 10.6311 mL | 21.2621 mL |
| 5 mM | 425.2 μL | 2.1262 mL | 4.2524 mL |
| 10 mM | 212.6 μL | 1.0631 mL | 2.1262 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。
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