| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
Tracarzolate enhances the binding of [3H]-flunitrazepam to benzodiazepine receptors in mammalian brain tissue [1]. Tracarzolate enhances the binding of [3H]-GABA to its receptors in mammalian brain tissue [1]. Tracarzolate enhances the binding of [3H]-flunitrazepam to brain tissue [2]. Tracarzolate enhances the binding of GABA to rat meningeal components [2].
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| ln Vivo |
Tracarzolate (10-80 mg/kg; intraperitoneal; oral; single dose) showed dose-dependent anxiolytic activity in an electric shock-induced drinking inhibition test in rats, with a relative potency of about 1/4 to 1/2 that of clozapine [1]. At all tested doses, tracarzolate (5-40 mg/kg; intraperitoneal; oral; single dose) did not produce statistically significant anxiolytic activity in the Geller conflict test in rats [1]. Tracarzolate (40-80 mg/kg; oral; once daily; for 12 days) did not show tolerance to anxiolytic activity after being administered once daily for 12 days in rats at doses of 40 or 80 mg/kg [1]. Tracarzolate (25-200 mg/kg; oral; single dose) showed dose-dependent anxiolytic activity in a mouse exploratory conflict test, with the lowest effective dose being 25 mg/kg (oral) [1]. Tracarzolate (intraperitoneal injection; single dose) has a weak antagonistic effect on metronidazole and bispus-induced convulsions in mice, with intraperitoneal ED50s of 27.7 mg/kg and 22.5 mg/kg, respectively [1]. Tracarzolate (oral; single dose) impairs rotarod test performance in mice at high doses, with an oral ED50 of 117.1 mg/kg [1]. Tracarzolate (oral; single dose) does not impair rotarod test performance in rats when administered via gastric infusion at doses up to 400 mg/kg [1]. Tracarzolate (12.5–100 mg/kg; oral; single dose) does not significantly exacerbate ethanol-induced rotarod test impairment in mice even when administered via gastric infusion at doses up to 100 mg/kg [1]. Tracarzolate (12.5-50 mg/kg; oral; single dose) prolonged ethanol-induced sleep time in mice at oral doses of 25 mg/kg and above, with its minimum effective dose being comparable to the minimum effective dose for anxiolytic effects [1]. Tracarzolate (5-10 mg/kg; oral; single dose) enhanced the anxiolytic activity of chlordiazepoxide in a shock-induced feeding depression rat model [1]. Tracarzolate (12.5 mg/kg; intraperitoneal; single dose) enhanced the anticonvulsant activity of chlordiazepoxide in mice, reducing the ED50 of chlordiazepoxide by approximately 6-fold [1]. Tracarzolate (20-40 mg/kg; intraperitoneal; single dose) did not increase water intake in non-dehydrated rats, nor did intraperitoneal doses of 20 or 40 mg/kg, suggesting that its anxiolytic activity was independent of driving force [1].
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| Animal Protocol |
Animal/Disease Models:Wistar mice (male, 180-220 g) [1]
Doses: 10 mg/kg; 20 mg/kg; 40 mg/kg; 80 mg/kg Route of Administration: Intraperitoneal injection; Oral administration; Single dose Experimental Results: Resulted in a statistically significant dose-dependent increase in the average number of electric shocks. Its relative potency was approximately 1/4 to 1/2 that of chlordiazepoxide. Animal/Disease Models:Sprague-Dawley mice (male, 240-260 g, maintained at approximately 80% of their free-feeding body weight)[1] Doses: 5 mg/kg; 10 mg/kg; 20 mg/kg; 40 mg/kg Route of Administration: Intraperitoneal injection; Oral administration; Single dose Experimental Results: Intraperitoneal injection of 5 mg/kg, 10 mg/kg, and 20 mg/kg increased the penalty response by 7.7%, 2.1%, and 29.0%, respectively, but the differences were not statistically significant. Oral administration of 40 mg/kg increased the penalty response by 126.6%, but this did not reach statistical significance. Animal/Disease Models:Wistar (male, 180-220 g)[1] Doses: 40 mg/kg; 80 mg/kg Route of Administration: Oral; daily; 12 days Experimental Results: It maintained statistically significant anxiolytic activity with an average of 9.95 (40 mg/kg) and 10.16 (80 mg/kg) electric shocks received. Animal/Disease Models:Swiss-Webster (male, 18-25 g) [1] Doses: 25 mg/kg; 50 mg/kg; 100 mg/kg; 200 mg/kg Route of Administration: Oral; single dose Experimental Results: Oral administration achieved the minimum effective dose (MED) of 25 mg/kg, which significantly increased the average number of electric shocks. Animal/Disease Models:Swiss-Webster (male, 18-25 g) [1] Doses: ED50 27.7 mg/kg (95% confidence interval 19.4-38.4) Route of Administration: Intraperitoneal injection; single dose Experimental Results: Intraperitoneal injection of ED50 of 27.7 mg/kg (95% confidence interval 19.4-38.4) prevented methazolate-induced seizures. Animal/Disease Models:Swiss-Webster (male, 18-25 g) [1] Doses: ED50 22.5 mg/kg (95% confidence interval 8.9-51.9) Route of Administration: Intraperitoneal injection; single dose Experimental Results: Intraperitoneal injection of ED50 at 22.5 mg/kg (95% confidence interval 8.9-51.9) prevented biscourin-induced seizures. Animal/Disease Models:Swiss-Webster (male, 18-25 g) [1] Doses: ED50 117.1 mg/kg (95% confidence interval 85.0-191.1) Route of Administration: Oral; single dose Experimental Results: The ED50 of oral administration was 117.1 mg/kg (95% confidence interval 85.0-191.1), which resulted in impaired rotator motility. Animal/Disease Models:Wistar (male, 180-220 g) [1] Doses: 400 mg/kg Route of Administration: Oral; single dose Experimental Results: Oral administration at the highest test dose of 400 mg/kg did not significantly impair rotator test performance. Animal/Disease Models:Swiss-Webster (male, 18–25 g) [1] Doses: 12.5 mg/kg; 25 mg/kg; 50 mg/kg; 100 mg/kg Route of Administration: Oral; Single dose Experimental Results: No significant enhancement of ethanol-induced rotarod test injury; ataxia rates were 0.0%, 0.0%, 16.7%, and 16.7%, respectively. Animal/Disease Models:Swiss-Webster (male, 18-25 g) [1] Doses: 12.5 mg/kg; 25 mg/kg; 50 mg/kg Route of Administration: Oral; Single dose Experimental Results: The minimum effective dose of 25 mg/kg was reached orally, which significantly prolonged ethanol-induced sleep time to 59.9 minutes. Oral administration of 50 mg/kg prolonged sleep time to 95.0 minutes. Oral administration of 12.5 mg/kg had no significant effect. Animal/Disease Models:Wistar (male, 180-220 g) [1] Doses: 5 mg/kg; 10 mg/kg Route of Administration: Oral Experimental Experimental Results: When used in combination with chlordiazepoxide 2.5 mg/kg orally (the dose was insufficient when used alone), it significantly increased the average number of electric shocks, and its enhancing effect was greater than the sum of the effects of each drug alone. Animal/Disease Models:Swiss-Webster (male, 18-25 g) [1] Doses: 12.5 mg/kg Route of Administration: Intraperitoneal injection Experimental Results: Reducing the ED50 of chlordiazepoxide's protective effect against metronidazole-induced convulsions from 4.9 mg/kg orally to 0.8 mg/kg orally increased the efficacy of chlordiazepoxide by about 6 times. Animal/Disease Models:Wistar (male, 180-220 g) [1] Doses: 20 mg/kg; 40 mg/kg Route of Administration: Intraperitoneal injection Experimental Results: No increase in water intake; the average number of licks was 246.5 and 222.14, respectively, which were not significantly different from the control group. |
| References |
| Molecular Formula |
C16H24N4O2
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|---|---|
| Molecular Weight |
304.39
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| CAS # |
41094-88-6
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| Appearance |
Typically exists as solids at room temperature
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| SMILES |
O=C(OCC)C1=C(N=C2C(C=NN2CC)=C1NCCCC)C
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| Synonyms |
ICI 136753
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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 | 3.2853 mL | 16.4263 mL | 32.8526 mL | |
| 5 mM | 0.6571 mL | 3.2853 mL | 6.5705 mL | |
| 10 mM | 0.3285 mL | 1.6426 mL | 3.2853 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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