| Size | Price | Stock | Qty |
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| 1g |
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| Other Sizes |
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| ln Vitro |
When lipopolysaccharide (LPS) is applied to mouse microglial cell line BV2 cells, nitric oxide (NO) release and proinflammatory cytokine production are inhibited by bromisoval (BU). Interferon regulatory factor 1 (IRF1) expression and the phosphorylation of signal transducer and activator of transcription 1 (STAT1) induced by lipopolysaccharide (LPS) are inhibited by bromisoval. The NO release was not as substantially inhibited by the Janus kinase 1 (JAK1) inhibitor filgotinib as it was by Bromisoval; nevertheless, filgotinib virtually totally prevented LPS-induced STAT1 phosphorylation. The inhibitory impact of Bromisoval on LPS-induced NO was not affected by JAK1, STAT1, or IRF1 knockdown. Bromisoval and filgotinib work together to synergistically decrease NO release. Rotenone, an inhibitor of mitochondrial complex I, has a less significant inhibitory effect on the expression of pro-inflammatory mediators than bromisoval, but it does not prevent STAT1 phosphorylation or IRF1 expression. Rotenone and bromisoval both lower intracellular ATP (iATP) levels to a comparable degree. Rotenone and filgotinib together exhibited a potency comparable to that of bromisoval in inhibiting the release of NO in LPS-treated BV2 cells [1].
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| ln Vivo |
Of each series, carbobromal and bromisoval (Bromvaletone) are the most powerful central depressants. Following intraperitoneal injection in male mice, the inhibitory activity (ISD50 value) and acute toxicity (LD50 value) of bromisoval were 0.35 (0.30-0.39) and 3.25 (2.89-3.62) mmol/kg, respectively [2].
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| References | |
| Additional Infomation |
2-bromo-N-carbamoyl-3-methylbutanamide is an N-acylurea that is urea in which one of the hydrogens is replaced by a 2-bromo-3-methybutanoyl group. It is a N-acylurea and an organobromine compound.
A sedative and mild hypnotic with potentially toxic effects. |
| Molecular Formula |
C6H11BRN2O2
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|---|---|
| Molecular Weight |
223.07
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| Exact Mass |
222
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| CAS # |
496-67-3
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| PubChem CID |
2447
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| Appearance |
White to off-white solid powder
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| Density |
1.504g/cm3
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| Melting Point |
152 °C
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| Index of Refraction |
1.514
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| LogP |
1.692
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
|
| Heavy Atom Count |
11
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| Complexity |
170
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| Defined Atom Stereocenter Count |
0
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| SMILES |
BrC([H])(C(N([H])C(N([H])[H])=O)=O)C([H])(C([H])([H])[H])C([H])([H])[H]
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| InChi Key |
CMCCHHWTTBEZNM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C6H11BrN2O2/c1-3(2)4(7)5(10)9-6(8)11/h3-4H,1-2H3,(H3,8,9,10,11)
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| Chemical Name |
2-bromo-N-carbamoyl-3-methylbutanamide
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| Synonyms |
Isobromyl Bromaral Bromisoval bromovalerylureaBRN1773255 BRN 1773255 BRN-1773255
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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 : ~300 mg/mL (~1344.87 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 7.5 mg/mL (33.62 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 75.0 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: ≥ 7.5 mg/mL (33.62 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 75.0 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: ≥ 7.5 mg/mL (33.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4829 mL | 22.4145 mL | 44.8290 mL | |
| 5 mM | 0.8966 mL | 4.4829 mL | 8.9658 mL | |
| 10 mM | 0.4483 mL | 2.2414 mL | 4.4829 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05799001 | RECRUITING | Behavioral: Dance therapy | Dementia | Centre Hospitalier Emile Roux | 2023-03-08 | Not Applicable |
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