| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
BDZ-g specifically targets the AMPA receptor, which is a type of ionotropic glutamate receptor. It acts as an antagonist, blocking the receptor's activity. BDZ-g is a potent inhibitor of both the closed-channel and open-channel conformations of all four homomeric AMPA receptor channels, as well as two GluA2R-containing complex AMPA receptor channels.
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| ln Vitro |
In vitro, BDZ-g potently blocks AMPA receptor-mediated currents. It inhibits both the closed-channel and open-channel conformations of the AMPA receptor, indicating a complex mechanism of action that stabilizes the receptor in a non-conductive state. Its high selectivity for AMPA receptors over other iGluR subtypes makes it a valuable tool for studying AMPA receptor function.
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| ln Vivo |
Specific in vivo data for BDZ-g are not extensively documented in the available literature. However, as a potent and selective AMPA receptor antagonist, it has the potential for studying various neurological disorders involving excessive activity of AMPA receptors, such as epilepsy, neurodegenerative diseases, and stroke. Its in vivo effects would likely involve reducing excitatory neurotransmission in the brain.
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| Enzyme Assay |
The in vitro receptor binding assay for BDZ-g involves measuring its affinity for the AMPA receptor. This is typically done using radioligand binding assays with membrane preparations from rat brain or from cells expressing recombinant AMPA receptors. A radiolabeled AMPA receptor ligand, such as [³H]-AMPA, is used in competition binding experiments to determine the Ki of BDZ-g.
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| Cell Assay |
In vitro cellular assays for BDZ-g are performed using electrophysiological techniques, such as patch-clamp, on neurons or cells expressing AMPA receptors. The ability of BDZ-g to block AMPA-induced currents is measured. Cells are voltage-clamped, and the reduction in current amplitude upon application of AMPA in the presence of BDZ-g is quantified to determine its potency (IC50) and mechanism of action.
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| Animal Protocol |
In vivo animal experiments for BDZ-g would likely involve rodent models of neurological disorders. For example, in a model of epilepsy, BDZ-g could be administered (e.g., intraperitoneally) to test its ability to reduce seizure frequency or severity. In stroke models, it could be tested for its neuroprotective effects by reducing excitotoxicity. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic properties of BDZ-g have not been extensively detailed in the available literature. As a small molecule with a molecular weight of 407.49 g/mol and a LogP of 4.6, it is expected to have high membrane permeability and the ability to cross the blood-brain barrier. The compound is soluble in DMSO, which is typical for such research compounds.
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| Toxicity/Toxicokinetics |
Specific toxicity data for BDZ-g are not readily available in the public domain. Material safety data sheets (MSDS) classify it as not a hazardous substance or mixture, but standard laboratory precautions should be followed. As with all research chemicals, it is recommended to avoid inhalation, contact with eyes and skin, and to use it only in areas with appropriate exhaust ventilation.
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| References | |
| Additional Infomation |
BDZ-g is a research chemical that is not an approved drug. It is part of a class of compounds known as 2,3-benzodiazepines, which are non-competitive AMPA receptor antagonists. It is used as a tool to study the role of AMPA receptors in excitatory synaptic transmission and in various neuropathologies. Its high selectivity and potency make it a superior tool compared to older, less selective AMPA antagonists.
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| Molecular Formula |
C21H21N5O2S
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|---|---|
| Molecular Weight |
407.488742589951
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| Exact Mass |
407.141
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| CAS # |
732278-52-3
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| PubChem CID |
10250827
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| Appearance |
White to yellow solid powder
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| LogP |
4.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
29
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| Complexity |
636
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| Defined Atom Stereocenter Count |
1
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| SMILES |
S1C(C)=NN=C1N1[C@@H](C)CC2C=C3C(=CC=2C(C2C=CC(=C(C)C=2)N)=N1)OCO3
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| InChi Key |
DBDUGNPURSLMPS-GFCCVEGCSA-N
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| InChi Code |
InChI=1S/C21H21N5O2S/c1-11-6-14(4-5-17(11)22)20-16-9-19-18(27-10-28-19)8-15(16)7-12(2)26(25-20)21-24-23-13(3)29-21/h4-6,8-9,12H,7,10,22H2,1-3H3/t12-/m1/s1
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| Chemical Name |
2-methyl-4-[(8R)-8-methyl-7-(5-methyl-1,3,4-thiadiazol-2-yl)-8,9-dihydro-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl]aniline
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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 | 2.4540 mL | 12.2702 mL | 24.5405 mL | |
| 5 mM | 0.4908 mL | 2.4540 mL | 4.9081 mL | |
| 10 mM | 0.2454 mL | 1.2270 mL | 2.4540 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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