ANA 12
Catalog No.: GC11486Purity:>99.50%
ANA 12 هو مضاد TrkB قوي وانتقائي ، ويرتبط بـ TrkBECD-Fc بـ Kd 12 ميكرومتر.
المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.
Cas No.: 219766-25-3
10mM (in 1mL DMSO)In Stock
$70.00
1
5mgIn Stock
$52.00
1
25mgIn Stock
$152.00
1
100mgIn Stock
$430.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $70.00 | In Stock | 1 | |
| 5mg | $52.00 | In Stock | 1 | |
| 25mg | $152.00 | In Stock | 1 | |
| 100mg | $430.00 | In Stock | 1 |
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المراجع (Citations)
2 publicationsمنشورات الباحثين الذين استخدموا هذا المنتجالوصف (Description)
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.
البروتوكول (Protocol)
| 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: | |
وثائق المنتج (Product Documents)
Purity:>99.50%Appearance:A solid
الخصائص الكيميائية (Chemical Properties)
رقم CAS
219766-25-3
الاسم الكيميائي
N-(2-((2-oxoazepan-3-yl)carbamoyl)phenyl)benzo[b]thiophene-2-carboxamide
SMILES
O=C(NC1CCCCNC1=O)C2=CC=CC=C2NC(C3=CC4=CC=CC=C4S3)=O
الصيغة الجزيئية
C22H21N3O3S
الوزن الجزيئي
407.49
الذوبانية
≥ 10.2mg/mL in DMSO with gentle warming
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.
الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية
g/mol
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