| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
Tracazolate HCl targets GABAA receptors, the major inhibitory neurotransmitter receptors in the central nervous system. It is a subtype-selective GABAA receptor modulator that potentiates or inhibits recombinant GABAA function. Tracazolate HCl is selective for the β3 subunit and enhances both α1β1γ2s (EC50=13.2 μM) and α1β3γ2 (EC50=1.5 μM) receptor combinations.
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| ln Vitro |
Hydrochronide α1β1ε (EC50=4.0 μM), α1β3ε (EC50=1.2 μM), α1β3 (EC50=2.7 μM), and α6β3γ (EC50=1.1 μM) are inhibited by Tracazolate (ICI 136753). Trazazolate sensitivity is increased when Asn (the β3 homologue) replaces Ser265 within the β1 subunit; tracazolate sensitivity is decreased when Ser is replaced with Asn. Adenosine receptors, phosphodiesterase, and gamma-aminobutyric acid GABAA receptors are all interacting with tracazolate hydrochloride [1]. In oocytes, the maximal current amplitude is increased and the sensitivity of GABAA receptors containing α1β2δ is enhanced by tracazolate hydrochloride (10 μM) [2].
In vitro, Tracazolate HCl is a potent GABAA receptor modulator. It enhances GABA-mediated chloride influx at GABAA receptors. It is selective for β3-containing receptors, with EC50 values of 13.2 μM for α1β1γ2s and 1.5 μM for α1β3γ2. These in vitro properties make Tracazolate HCl a valuable tool for studying GABAA receptor pharmacology and subunit selectivity. |
| ln Vivo |
In vivo, Tracazolate HCl is a non-benzodiazepine compound that exhibits anxiolytic-like effects. It modulates GABAA receptors, enhancing GABA-mediated neuronal inhibition. These properties suggest potential for treating anxiety disorders. However, detailed in vivo efficacy data are limited in publicly available sources.
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| Enzyme Assay |
The in vitro receptor binding assay for Tracazolate HCl involves measuring its binding affinity to GABAA receptor subtypes. The compound is incubated with membranes expressing different GABAA receptor combinations (e.g., α1β1γ2s, α1β3γ2) in the presence of a radiolabeled GABAA receptor ligand (e.g., [3H]muscimol or [3H]flunitrazepam). Binding affinity is determined using competition binding assays. Functional modulation can be assessed by measuring GABA-induced chloride influx or electrophysiological responses.
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| Cell Assay |
The in vitro cell-based assay for Tracazolate HCl involves culturing cells expressing GABAA receptors (e.g., recombinant cell lines or primary neurons) and treating them with the compound to assess effects on receptor function. Cells are treated with Tracazolate HCl at various concentrations in the presence of GABA, and chloride influx is measured using fluorescent chloride indicators (e.g., MQAE) or patch-clamp electrophysiology. Subtype selectivity is assessed by comparing EC50 values across different receptor combinations. Cell viability is assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies for Tracazolate HCl have been conducted in models of anxiety. Rodents are administered Tracazolate HCl, and anxiolytic-like effects are assessed using behavioral tests such as the elevated plus maze, open field test, or light-dark box test. Standard protocols for anxiolytic compound evaluation are employed. However, detailed data are limited in publicly accessible sources.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Tracazolate HCl have not been extensively characterized. As a small molecule, it is expected to have moderate oral bioavailability. Tracazolate HCl is soluble in 0.1 M HCl. The compound has a molecular formula of C16H24N4O2 (free base) and a molecular weight of 304.39 (free base). Detailed PK parameters such as half-life, Cmax, and bioavailability are not available from publicly accessible sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of Tracazolate HCl has not been systematically evaluated. As a GABAA receptor modulator, its primary safety concerns would relate to central nervous system effects, including sedation, ataxia, and dependence potential. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No specific toxicity data are available.
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| References | |
| Additional Infomation |
Tracazolate HCl is a research compound and has not been approved for clinical use. It is a potent GABAA receptor modulator and a pyrazolopyridine derivative that exhibits anxiolytic-like effects. Tracazolate HCl is selective for β3 and enhances both α1β1γ2s (EC50=13.2 μM) and α1β3γ2 (EC50=1.5 μM). It modulates GABAA receptors, enhancing GABA-mediated chloride influx and neuronal inhibition.
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| Molecular Formula |
C16H25CLN4O2
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| Molecular Weight |
340.848302602768
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| Exact Mass |
340.166
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| Elemental Analysis |
C, 56.38; H, 7.39; Cl, 10.40; N, 16.44; O, 9.39
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| CAS # |
1135210-68-2
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| Related CAS # |
41094-88-6;1135210-68-2 (HCl);
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| PubChem CID |
24871267
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
23
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| Complexity |
366
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCNC1=C2C=NN(C2=NC(=C1C(=O)OCC)C)CC.Cl
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| InChi Key |
TUIXDPUEMQXVHO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H24N4O2.ClH/c1-5-8-9-17-14-12-10-18-20(6-2)15(12)19-11(4)13(14)16(21)22-7-3;/h10H,5-9H2,1-4H3,(H,17,19);1H
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| Chemical Name |
1H-Pyrazolo(3,4-b)pyridine-5-carboxylic acid, 4-(butylamino)-1-ethyl-6-methyl-, ethyl ester, hydrochloride
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| Synonyms |
ICI 136753; ICI136753; ICI-136753; Tracazolate; Tracazolate HCl;
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~125 mg/mL (~366.73 mM)
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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 | 2.9338 mL | 14.6692 mL | 29.3384 mL | |
| 5 mM | 0.5868 mL | 2.9338 mL | 5.8677 mL | |
| 10 mM | 0.2934 mL | 1.4669 mL | 2.9338 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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