Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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ln Vitro |
The affinity of gidazepam for GABA RC is notably lower than that of br-norzepam, phenazepam, and 3-hydroxyfenazepam. The benzodiazepine receptor-specific ligand diazepam exhibits varying values of the binding inhibition constant (Ki). The Ki value for gidazepam is 2,200±50 nM[1].
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ln Vivo |
Ten groups of five mice each were used to administer oral treatments of gidazepam (GDZ, 1 mg/kg), ester 1 (175 mg/kg), ester 2 (20 mg/kg), ester 3 and 4 (200 mg/kg), or a combination of gidazepam and esters 1-4. Within three hours of oral treatment, all GABA esters containing monoterpenes demonstrated anticonvulsant effects, as indicated by an increase in the values of tonic extension (DTE) and produced clonic tonic convulsions (DCTC). With comparable DCTC and DTE values of 250% and 215%, respectively, gidazepam (1 mg/kg) was shown to prevent epileptic seizures; when administered in combination with its esters 5-7, gidazepam and their combined administration may boost anticonvulsant activity as compared with each drug alone [1].
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References |
[1]. N. Ya Golovenko, et al. Pharmacodynamical and Neuroreceptor Analysis of the Permeability of the Blood-Brain Barrier for Derivatives of 1,4-Benzodiazepine. Neurophysiology, Vol. 46, No. 3, June, 2014.
[2]. Nesterkina M, et al. Synthesis and Pharmacological Properties of Novel Esters Based on Monocyclic Terpenes and GABA. Pharmaceuticals (Basel). 2016 Jun 13;9(2). pii: E32 |
Molecular Formula |
C17H15N4O2BR
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Molecular Weight |
387.2306
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CAS # |
129186-29-4
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Related CAS # |
Gidazepam-d5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(NN)CN1C(CN=C(C2=CC=CC=C2)C3=CC(Br)=CC=C31)=O
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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) |
DMSO : ~250 mg/mL (~645.61 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 | 2.5824 mL | 12.9122 mL | 25.8244 mL | |
5 mM | 0.5165 mL | 2.5824 mL | 5.1649 mL | |
10 mM | 0.2582 mL | 1.2912 mL | 2.5824 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.