ANA-12

CatalogusnummerS7745 Batch:S774501

Afdrukken

Technische gegevens

Formule

C22H21N3O3S
Moleculair gewicht 407.49 CAS-nr. 219766-25-3
Oplosbaarheid (25°C)* In vitro DMSO 37 mg/mL (90.79 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Voeg oplosmiddelen afzonderlijk en in volgorde toe aan het product.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml betekent licht oplosbaar of onoplosbaar.
* Houd er rekening mee dat Selleck de oplosbaarheid van alle verbindingen intern test en de werkelijke oplosbaarheid enigszins kan afwijken van gepubliceerde waarden. Dit is normaal en is te wijten aan lichte batch-tot-batch variaties.
* Verzending op kamertemperatuur (Stabiliteitstests tonen aan dat dit product zonder koelmaatregelen kan worden verzonden.)

Voorbereiden van stamoplossingen

Biologische activiteit

Beschrijving ANA-12 is een selectieve TrkB-antagonist met een Kd van respectievelijk 10 nM en 12 μM voor de hoge en lage affiniteitsplaatsen.
Doelen
TrkB
10 nM(Kd)
In vitro ANA-12 binds directly and selectively to TrkB and inhibits processes downstream of TrkB without altering TrkA and TrkC functions. In nnr5 PC12-TrkB cells, this compound prevents brain-derived neurotrophic factor (BDNF)-induced neurite outgrowth at concentrations as low as 10 nM. In DRG neurons, this chemical eliminates the effect of BDNF on increasing inward current.
In vivo In adult C57BL6/129SveV F1s mice, ANA-12 (0.5 mg/kg, i.p.) decreases TrKB activity in the brain and reduces the anxiety- and depression-related behaviors without affecting the neuron survival. In male C57BL/6 mice, this compound shows antidepressant-like effects on lipopolysaccharide-induced depression-like behavior. In male Sprague-Dawley rats, this chemical blocks the effect of medial nucleus tractus solitarius (mNTS) BDNF on reducing food intake. In male wild-type mice, it reverses ethanol intake and induces D3 receptor downregulation, but is ineffective in D3R-/- mice. In male CocSired rats, this compound reverses the diminished self-administration of cocaine.

Protocol (uit referentie)

Kinase-assay:

[1]
  • ANA-12 Binding assay

    Maxisorp ELISA 96-well plates are coated with various concentrations of Trk BECD -Fc, 20 mg/ml BSA, or 1 mg/mL IgG-Fc (polyclonal anti-TrkB) in a carbonate buffer (pH 9.6) overnight at 4°C. Plates are saturated with 0.5% BSA in PBS for 2 hours at room temperature and extensively washed in PBS-Tween 0.05%. Bodipy–ANA-12 is then incubated in 0.5% PBS-BSA for 1 hour at room temperature before the addition of BDNF in 0.5% PBS-BSA for another hour. After extensive washes in PBS-Tween 0.05%, the amount of bodipy–this compound bound is quantified by fluorescence at 520 ± 10 nm. Detectability range for extrapolation analysis is assessed by coating ELISA plates with bodipy–this chemical and reading fluorescence at 520 ± 10 nm.
Celassay:

[1]
  • Cellijnen

    nnr5 PC12–TrkA, nnr5 PC12–TrkB, and nnr5 PC12–TrkC cells

  • Concentraties

    ~100 μM

  • Incubatietijd

    ~3 days

  • Methode

    Modulation of neurite outgrowth by molecules is assessed in nnr5 PC12–TrkB, –TrkA, and –TrkC cells after addition of BDNF (1 nM), NGF (2 nM), and NT-3 (10 nM), respectively. The number of cells bearing neurites longer than 2 cells in diameter in each counting field is microscopically determined (2 fields per well, 3 wells per condition). Counting is performed blind each 24 hours for 3 days.
Dierstudie:

[1]
  • Dierlijke modellen

    Adult C57BL6/129SveV F1s mice

  • Doseringen

    0.5 mg/kg

  • Toediening

    i.p.

Referenties

  • http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3083767/
  • https://pubmed.ncbi.nlm.nih.gov/24611998/
  • https://pubmed.ncbi.nlm.nih.gov/25628381/
  • https://pubmed.ncbi.nlm.nih.gov/22374757/
  • https://pubmed.ncbi.nlm.nih.gov/24584330/
  • https://pubmed.ncbi.nlm.nih.gov/23242310/

Klantproductvalidatie

Maternal exercise ameliorated sevoflurane-induced neuronal cell loss and decreased dendritic spine density, blocked by TrkB inhibition. Nissl staining and Golgi staining were performed after behavior tests (n = 3). (A) Nissl staining in the CA1 region of hippocampus under ×400. (B) Neuronal density ratio changes. (C) Golgi staining in the CA1 of hippocampus under ×1000. (D) Histograms represented the number of dendritic spines/10 μm. Values are mean ± S.E.M. *p < 0.05, compared with Ctrl group; **p < 0.01, compared with Ctrl group; ##p < 0.01, compared with Sevo group; ∧∧p < 0.01, compared with Sevo + ME group. One-way analysis of variance followed by Tukey post hoc multiple comparison tests was used for data analysis.

Gegevens van [ , , Front Cell Neurosci, 2018, doi:10.3389/fncel.2018.00122 ]

Total Ca2+/calmodulin-dependent protein kinase II (CaMKII) (pan) and phosphorylated (p-)CaMKII protein expression with representative Western blot images and p-CaMKII-to-CaMKII (pan) ratio in the noninfarct area of the left ventricle (LV) of rats at 5 wk postmyocardial infarction (post-MI) with or without exercise training or ANA-12 treatment. Representative Western blot images of p-CaMKII and CaMKII (pan) with GAPDH as the loading control (A), p-CaMKII (B) and CaMKII (pan) (C) protein expression, and the p-CaMKII-to-CaMKII (pan) ratio in the LV of sham and MI rats with or without exercise training or ANA-12 treatment (D) are shown. Values are means ± SE. Sham group, n = 10; sedentary MI with vehicle treatment (Sed-MI-Veh) group, n = 8; exercise training with MI and vehicle treatment (ExT-MI-Veh) group, n = 9; and exercise training with MI and ANA-12 treatment (ExT-MI-ANA-12) group, n = 8. All bands were normalized to GAPDH and are shown as fold values of the sham group. Statistical analysis was done by one-way ANOVA followed by a Bonferroni post hoc test. For p-CaMKII, F = 6.1, P < 0.01; for CaMKII (pan), F = 1.5, not significant; for p-CaMKII/CaMKII (pan), F = 12.9, P < 0.001. **P < 0.01, and ***P < 0.001 vs. the sham group.

Gegevens van [ , , Am J Physiol Heart Circ Physiol, 2018, doi:10.1152/ajpheart.00245.2018 ]

(D) when examined on day 11 after stress withdrawal. *p < 0.05 and ***p < 0.001 comparison to vehicle-treated stressed rats, and #p < 0.05 and ###p < 0.001 comparison to apelin-13-treated stressed rats. CWIRS, chronic water-immersion restraint stress; Apelin, apelin-13.

Gegevens van [ , , Neuroscience, 2018, 390:151-159 ]

Sellecks ANA-12 Is geciteerd door 47 Publicaties

A Novel Gastrodin Derivative with Neuroprotection Promotes NGF-Mimic Activity by Targeting INSR and ACTN4 to Activate PI3K/Akt Signaling Pathway in PC12 Cells [ Antioxidants (Basel), 2025, 14(3)344] PubMed: 40227445
A novel synthetic 3,4,5-tri-feruloylquinic acid enhances learning and memory via neurotrophin signaling in an aging model senescence-accelerated prone 8 mice [ Geroscience, 2025, 10.1007/s11357-025-01783-7] PubMed: 40699486
ANA-12 Targets and Inhibits BDNF/TrkB Signaling to Alleviate Pain Behaviors in Rheumatoid Arthritis Mice [ Neurochem Res, 2025, 50(4):234] PubMed: 40673956
Neuronal FSTL4 negatively regulates BDNF-mediated neuron-glioma interaction [ Neurochem Int, 2025, 191:106072] PubMed: 41082941
Club cell-derived brain-derived neurotrophic factor regulates murine airway mechanics and mucin production in response to IL-13 in a sex-dependent manner [ Front Physiol, 2025, 16:1578553] PubMed: 40626045
Allium Macrostemon Bge. Attenuates the Cognitive Decline of Aging Mice by Enhancing BDNF/TrkB Pathway [ Food Sci Nutr, 2025, 13(3):e70010] PubMed: 40027296
Isoform-Specific Roles of NTRK2 in Pulmonary Vascular Regeneration [ bioRxiv, 2025, 2025.05.11.653351] PubMed: 40463206
Progressive reduction of nuclear receptor Nr4a1 mediates age-dependent cognitive decline [ Alzheimers Dement, 2024, 10.1002/alz.13819] PubMed: 38605605
HDAC6-dependent deacetylation of NGF dictates its ubiquitination and maintains primordial follicle dormancy [ Theranostics, 2024, 14(6):2345-2366] PubMed: 38646645
A rare olive compound oleacein functions as a TrkB agonist and mitigates neuroinflammation both in vitro and in vivo [ Cell Commun Signal, 2024, 22(1):309] PubMed: 38835076

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NIET VOOR HUMANE, VETERINAIRE DIAGNOSTISCHE OF THERAPEUTISCHE DOELEINDEN.