| Size | Price | |
|---|---|---|
| 5mg | ||
| Other Sizes |
| Targets |
The primary molecular targets of HZ166 are GABAA receptors containing α2 and α3 subunits. These receptors are benzodiazepine-sensitive and mediate anxiolytic, muscle relaxant, and analgesic effects. HZ166 binds to the benzodiazepine site at the interface of α and γ subunits and acts as an agonist, enhancing GABA-induced chloride currents. It shows preferential activity at α2- and α3-containing receptors over α1- and α5-containing receptors. The alkyne group allows for click chemistry conjugation for imaging or affinity labeling.
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|---|---|
| ln Vitro |
In vitro activity of HZ166 has been characterized using radioligand binding assays and electrophysiological recordings. In binding assays with recombinant GABAA receptors, HZ166 displaces [3H]flunitrazepam with higher affinity for α2- and α3-containing receptors than for α1- and α5-containing receptors. In patch clamp recordings, HZ166 enhances GABA-induced currents in a concentration-dependent manner. The compound shows functional selectivity for α2- and α3-containing receptors.
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| ln Vivo |
In vivo activity of HZ166 has been evaluated in rodent models of anxiety and pain. In the elevated plus maze and light-dark box tests, HZ166 produces anxiolytic-like effects. In models of neuropathic pain, HZ166 reduces mechanical allodynia and thermal hyperalgesia. These effects are mediated by α2- and α3-containing GABAA receptors. HZ166 shows reduced sedative and ataxic effects compared to non-selective benzodiazepines.
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| Enzyme Assay |
In vitro binding assays for HZ166 use membranes from cells expressing recombinant GABAA receptor subtypes (α1β2γ2, α2β2γ2, α3β2γ2, α5β2γ2). Radioligand [3H]flunitrazepam is incubated with membranes and varying concentrations of HZ166. Bound radioactivity is separated by filtration and quantified. Ki values are calculated for each receptor subtype.
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| Cell Assay |
In vitro cell experiments with HZ166 use HEK293 or CHO cells expressing recombinant GABAA receptors. Cells are cultured in standard media and treated with HZ166 at concentrations ranging from 0.01 to 10 µM. Electrophysiological recordings are performed using patch clamp to measure GABA-induced currents. All experiments include diazepam as a positive control.
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| Animal Protocol |
In vivo animal experiments with HZ166 use rats or mice. HZ166 is dissolved in a suitable vehicle and administered by intraperitoneal injection or oral gavage at doses ranging from 0.1 to 10 mg/kg. For anxiety models, the elevated plus maze and light-dark box tests are used. For pain models, mechanical allodynia is assessed by von Frey testing. All procedures follow institutional animal care guidelines.
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| References |
| Molecular Formula |
C21H16N4O2
|
|---|---|
| Molecular Weight |
356.3773
|
| Exact Mass |
356.127
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| CAS # |
612527-56-7
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| PubChem CID |
10309028
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| Appearance |
Typically exists as solid at room temperature
|
| LogP |
2.9
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| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
27
|
| Complexity |
639
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(OCC)C1=C2N(C3=CC=C(C=C3C(C4=NC=CC=C4)=NC2)C#C)C=N1
|
| InChi Key |
ZSEDMNMFODMQRD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H16N4O2/c1-3-14-8-9-17-15(11-14)19(16-7-5-6-10-22-16)23-12-18-20(21(26)27-4-2)24-13-25(17)18/h1,5-11,13H,4,12H2,2H3
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| Chemical Name |
ethyl 8-ethynyl-6-pyridin-2-yl-4H-imidazo[1,5-a][1,4]benzodiazepine-3-carboxylate
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| Synonyms |
HZ166; HZ 166; HZ-166
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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 | 2.8060 mL | 14.0300 mL | 28.0599 mL | |
| 5 mM | 0.5612 mL | 2.8060 mL | 5.6120 mL | |
| 10 mM | 0.2806 mL | 1.4030 mL | 2.8060 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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