ANA 12
目录号 : GC11486
ANA 12是一种小分子、非竞争性、高选择性TrkB受体拮抗剂（高亲和力位点：IC50 = 45.6nM；低亲和力位点：IC50 = 41.1μM）。
Cas No.:219766-25-3
Sample solution is provided at 25 µL, 10mM.
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ANA 12 is a small molecule, non-competitive, and highly selective TrkB receptor antagonist (high-affinity site: IC50 = 45.6nM; low-affinity site: IC50 = 41.1μM) [1]. ANA 12 blocks BDNF activation by binding to both high- and low-affinity sites of TrkB, thereby inhibiting multiple downstream signaling pathways (such as ERK/MAPK and PI3K), modulating neuroplasticity and behavior [2-3]. ANA 12 is primarily used to improve anxiety and depression-like symptoms [4].
In D283 and UW-228 cells, ANA 12 (5-30μM; 24-72h) selectively inhibits TrkB and suppresses the proliferation and viability of human cells [5]. In Schwann cells (SC) and B4B8 cells, ANA 12 (5μM; 4d) treatment reduced the mutual migration between SC and cancer cells and initiated more SC-associated cancer cell dissemination [6]. In SubG1 cells, ANA-12 (1μM; 24h) abolished the protective effect of brain-derived neurotrophic factor on astrocyte death induced by serum deprivation by increasing the percentage of SubG1 cells [7].
In C57BL/6 mouse, ANA 12 (0.5mg/kg; ip; 5d) treatment reduces ovarian volume and antral follicle number and increases the proportion of abnormal oocytes in 8-10 weeks-old mice [8]. In collagen-induced arthritis (CIA) mouse model, ANA 12 (0.5mg/kg; ip; 6d) treatment reduces pain behaviors and promotes motor function recovery [9].
References:
[1]. Cazorla M, Premont J, Mann A, et al. Identification of a low–molecular weight TrkB antagonist with anxiolytic and antidepressant activity in mice[J]. The Journal of clinical investigation, 2011, 121(5): 1846-1857.
[2]. Fang X, Yang C, Li S, et al. Brain-derived neurotrophic factor-TrkB signaling in the medial prefrontal cortex plays a role in the anhedonia-like phenotype after spared nerve injury[J]. European archives of psychiatry and clinical neuroscience, 2020, 270(2): 195-205.
[3]. Vassoler F M, White S L, Schmidt H D, et al. Epigenetic inheritance of a cocaine-resistance phenotype[J]. Nature neuroscience, 2013, 16(1): 42-47.
[4]. Zhang J, Yao W, Dong C, et al. Comparison of ketamine, 7, 8-dihydroxyflavone, and ANA-12 antidepressant effects in the social defeat stress model of depression[J]. Psychopharmacology, 2015, 232(23): 4325-4335.
[5]. Thomaz A, Pinheiro K V, Souza B K, et al. Antitumor activities and cellular changes induced by TrkB inhibition in medulloblastoma[J]. Frontiers in Pharmacology, 2019, 10: 698.
[6]. Ein L, Mei C, Bracho O, et al. Modulation of BDNF–TRKB interactions on Schwann cell-induced oral squamous cell carcinoma dispersion in vitro[J]. Anticancer research, 2019, 39(11): 5933-5942.
[7]. Saba J, Turati J, Ramirez D, et al. Astrocyte truncated-TrkB mediates BDNF antiapoptotic effect leading to neuroprotection[J]. J Neurochem, 2018, 146: 686-702.
[8]. Liu B, Liu Y, Li S, et al. BDNF promotes mouse follicular development and reverses ovarian aging by promoting cell proliferation[J]. Journal of Ovarian Research, 2023, 16(1): 83.
[9]. Yuan M, Zhang L, Zheng Y, et al. ANA-12 Targets and Inhibits BDNF/TrkB Signaling to Alleviate Pain Behaviors in Rheumatoid Arthritis Mice[J]. Neurochemical Research, 2025, 50(4): 1-14.
ANA 12是一种小分子、非竞争性、高选择性TrkB受体拮抗剂（高亲和力位点：IC50 = 45.6nM；低亲和力位点：IC50 = 41.1μM） [1]。ANA 12通过结合TrkB的高亲和力位点和低亲和力位点来阻断BDNF活化，从而抑制多条下游信号通路（例如ERK/MAPK和PI3K），调节神经可塑性和行为 [2-3]。ANA 12主要用于改善焦虑和抑郁样症状 [4]。
在D283和UW-228细胞中，ANA 12（5-30μM；24-72h）选择性抑制TrkB，并抑制人类细胞的增殖和活力 [5]。在Schwann细胞（SC）和B4B8细胞中，ANA 12（5μM；4d）治疗可降低SC细胞与癌细胞之间的相互迁移，并启动更多SC细胞相关的癌细胞播散 [6]。在SubG1细胞中，ANA-12（1μM；24h）通过增加SubG1细胞的百分比，消除了脑源性神经营养因子对serum deprivation诱导的星形胶质细胞死亡的保护作用 [7]。
在C57BL/6小鼠中，ANA 12（0.5mg/kg；ip；5d）治疗可减少8-10周龄小鼠的卵巢体积和窦卵泡数量，并增加异常卵母细胞的比例 [8]。在胶原诱导性关节炎（CIA）小鼠模型中，ANA 12（0.5mg/kg；ip；6d）治疗可减轻疼痛行为并促进运动功能恢复 [9]。
| Cell experiment [1]: | |
Cell lines | D283 and UW-228 cells |
Preparation Method | ANA 12 was dissolved in dimethyl sulfoxide. Brain-derived neurotrophic factor (BDNF) was diluted in sterile ultrapure water at the stock solution of 1,000 ng/ml. Cells were treated with increasing concentrations of ANA 12 (5, 10, 20, or 30μM) or human recombinant BDNF (50ng/mL) in complete medium for 6, 24, 48, or 72h. The concentration of the vehicle DMSO was used as control and did not exceed 0.5% (v/v). |
Reaction Conditions | 5-30μM; 24-72h |
Applications | ANA 12 selectively inhibits TrkB and suppresses the proliferation and viability of human cells. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mouse |
Preparation Method | For the experiments in aged mice (35–37 weeks), female C57BL/6 mice were divided into two groups randomly. One group of mice was treated with rh-brain derived neurotrophic factor (BDNF) (1µg/200µL) by daily intraperitoneal (IP) injection for 10 days. In parallel, another group of mice was treated with 0.9% normal saline (a vehicle control, 200µL) by daily IP injection for 10 days. Similarly, for the experiments in normal reproductive age mice (8–10 weeks-old), female C57BL/6 mice were divided into two groups randomly. One group of mice was treated with ANA 12 (0.5mg/kg), which can block BDNF-TrkB signal, by daily IP injection for 5 days. Another group of mice was treated with 17% DMSO (a vehicle control, ~ 200µL) by daily IP injection for 5 days. |
Dosage form | 0.5mg/kg; ip; 5d |
Applications | ANA 12 treatment reduces ovarian volume and antral follicle number and increases the proportion of abnormal oocytes in 8-10 weeks-old mice. |
References: | |
| Cas No. | 219766-25-3 | SDF | |
| 化学名 | N-(2-((2-oxoazepan-3-yl)carbamoyl)phenyl)benzo[b]thiophene-2-carboxamide | ||
| Canonical SMILES | O=C(NC1CCCCNC1=O)C2=CC=CC=C2NC(C3=CC4=CC=CC=C4S3)=O | ||
| 分子式 | C22H21N3O3S | 分子量 | 407.49 |
| 溶解度 | ≥ 10.2mg/mL in DMSO with gentle warming | 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 | 2.454 mL | 12.2702 mL | 24.5405 mL |
| 5 mM | 490.8 μL | 2.454 mL | 4.9081 mL |
| 10 mM | 245.4 μL | 1.227 mL | 2.454 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 |
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| % 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.
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Quality Control & SDS
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- Purity: >99.50%
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