| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
TrkB (tropomyosin-related kinase B). HIOC is a potent and selective activator of the TrkB receptor, which belongs to the neurotrophin receptor family. By activating TrkB and downstream ERK signaling, HIOC promotes neuronal survival, reduces apoptosis, and provides neuroprotection. HIOC crosses the blood-brain barrier and the blood-retinal barrier, making it suitable for central nervous system and retinal applications. It has shown protective activity in animal models of retinal degeneration.
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| ln Vitro |
HIOC activates the TrkB/ERK pathway and reduces neuronal cell death in vitro. As a TrkB activator, it mimics the neurotrophic effects of brain-derived neurotrophic factor (BDNF) but is a small molecule that can cross biological barriers. The specific potency (EC50) for TrkB activation is not detailed in the reference sources, but HIOC is described as a potent and selective activator. HIOC reduces early brain damage after subarachnoid hemorrhage (SAH) in animal models.
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| ln Vivo |
The survival rate of RGC (retinal ganglion cells) following ONC (optic nerve crush) can be increased by HIOC (C57BL/6 mice, 50 mg/kg, IP, three times a week for two weeks) [3].
HIOC has been shown to attenuate early brain injury following subarachnoid hemorrhage (SAH) in animal models. It also shows protective activity in an animal model of light-induced retinal degeneration. By activating TrkB/ERK signaling and reducing neuronal cell death, HIOC provides neuroprotection in these disease models. The compound crosses the blood-brain and blood-retinal barriers, enabling its effects on CNS and retinal tissues. |
| Enzyme Assay |
Not explicitly detailed in reference sources. A typical TrkB activation assay involves incubating recombinant TrkB protein with HIOC and measuring receptor autophosphorylation using an anti-phospho-TrkB antibody in an ELISA or TR-FRET format. Alternatively, a cell-based assay uses TrkB-expressing cells treated with HIOC, followed by Western blot detection of phospho-TrkB and downstream signaling molecules (p-ERK).
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| Cell Assay |
Not explicitly detailed in reference sources. A cell-based TrkB activation assay uses SH-SY5Y neuroblastoma cells or primary cortical neurons expressing TrkB. Cells are treated with HIOC at various concentrations for 15-60 minutes. TrkB phosphorylation at tyrosine 515/816 and ERK phosphorylation are measured by Western blot. Neuronal survival is assessed by measuring apoptosis (caspase-3 activation) or by counting viable neurons after exposure to toxic stimuli.
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| Animal Protocol |
In the light-induced retinal degeneration model, animals are exposed to intense light to induce retinal damage. HIOC is administered (e.g., intraperitoneally or orally) before or after light exposure, and retinal function is assessed by electroretinography. Retinal histology and photoreceptor cell counts are analyzed. In the SAH model, HIOC is administered after inducing subarachnoid hemorrhage, and early brain injury is assessed by neurological scores, brain edema, and neuronal apoptosis.
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| ADME/Pharmacokinetics |
HIOC has a molecular weight of 301.34 and formula C16H19N3O3. It can cross the blood-brain barrier and blood-retinal barrier. For in vivo formulation, co-solvent systems (e.g., DMSO, Tween 80, and saline) can be used. Storage should be at -20degC as powder; in lyophilized form, it is stable for up to 36 months. In solution, it should be stored at -20degC and used within 1 month to prevent loss of potency.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for HIOC are provided in the reference sources. In the animal models studied, HIOC was administered at doses sufficient for neuroprotective effects without reported overt toxicity. However, comprehensive safety studies would be required for clinical development. The compound is for research use only.
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| References |
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| Additional Infomation |
HIOC is a research compound not yet approved for clinical use. It is a valuable tool for studying TrkB receptor biology and for validating TrkB activation as a therapeutic strategy for neurodegenerative and retinal diseases. By mimicking BDNF neurotrophic effects with a small molecule that can cross the blood-brain barrier, HIOC offers advantages over BDNF itself for therapeutic development. The compound is protected by patents.
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| Molecular Formula |
C16H19N3O3
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|---|---|
| Molecular Weight |
301.340363740921
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| Exact Mass |
301.142
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| CAS # |
314054-36-9
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| PubChem CID |
5012758
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
746.1±60.0 °C at 760 mmHg
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| Flash Point |
405.0±32.9 °C
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| Vapour Pressure |
0.0±2.6 mmHg at 25°C
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| Index of Refraction |
1.648
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| LogP |
-1.49
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
22
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| Complexity |
429
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZIMKJLALTRLXJO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19N3O3/c20-11-3-4-14-13(8-11)10(9-19-14)5-7-18-16(22)12-2-1-6-17-15(12)21/h3-4,8-9,12,19-20H,1-2,5-7H2,(H,17,21)(H,18,22)
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| Chemical Name |
N-[2-(5-hydroxy-1H-indol-3-yl)ethyl]-2-oxopiperidine-3-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3185 mL | 16.5926 mL | 33.1851 mL | |
| 5 mM | 0.6637 mL | 3.3185 mL | 6.6370 mL | |
| 10 mM | 0.3319 mL | 1.6593 mL | 3.3185 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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