| Size | Price | Stock | Qty |
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| 5mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
Two drugs that are thought to be competitive inhibitors of GABA binding to GABAA receptors are bucculline and gabazine (SR 95531). When it comes to stopping GABA-generated currents, gabazine works better than bicuculline. Its IC50 is roughly 0.2 μM, and for currents induced by 3 μM GABA, it has a Hill coefficient of 1.0. Gabazine decreased the current induced by 10 μM alphaxalone by roughly 30% when it came to receptors with the wild-type β2 subunit. The gabazine concentration (~0.2 μM) required to generate half of the largest block. Additionally, only a partial current blockage gated by 300 μM pentobarbital was induced by gabazine. Once more, the maximum reduction is roughly 30%, and roughly 0.15 μM of gabazine is needed to form half of the largest block [1].
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| References |
| Molecular Formula |
C15H17N3O3
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| Molecular Weight |
287.31378
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| Exact Mass |
367.053
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| CAS # |
104104-50-9
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| PubChem CID |
107895
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| Appearance |
White to off-white solid powder
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| Boiling Point |
474.4ºC at 760 mmHg
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| Melting Point |
200 ºC (ethanol )
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| Flash Point |
240.7ºC
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| Vapour Pressure |
8.33E-10mmHg at 25°C
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
451
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GFZHNFOGCMEYTA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H17N3O3.BrH/c1-21-12-6-4-11(5-7-12)13-8-9-14(16)18(17-13)10-2-3-15(19)20;/h4-9,16H,2-3,10H2,1H3,(H,19,20);1H
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| Chemical Name |
4-[6-imino-3-(4-methoxyphenyl)pyridazin-1-yl]butanoic acid;hydrobromide
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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) |
H2O : ~100 mg/mL (~271.57 mM)
DMSO : ≥ 75 mg/mL (~203.68 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.79 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 7.14 mg/mL (19.39 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4806 mL | 17.4028 mL | 34.8056 mL | |
| 5 mM | 0.6961 mL | 3.4806 mL | 6.9611 mL | |
| 10 mM | 0.3481 mL | 1.7403 mL | 3.4806 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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