| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
BBT targets pancreatic β-cells and the pathways involved in glucose-stimulated insulin secretion (GSIS). It acts through the cAMP/PKA pathway and L-type voltage-dependent Ca2+ channels/CaMK2 pathway to enhance insulin secretion. By protecting β-cells from cytokine- or STZ-induced cell death, BBT restores β-cell function and improves glucose homeostasis in type 2 diabetes models.
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| ln Vitro |
In vitro, BBT protects β-cells from cytokine- or STZ-induced cell death. It enhances glucose-stimulated insulin secretion (GSIS) through the cAMP/PKA and L-type voltage-dependent Ca2+ channel/CaMK2 pathways. These in vitro properties make BBT a valuable tool for studying β-cell function, insulin secretion, and diabetes pathogenesis.
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| ln Vivo |
In vivo, BBT exhibits anti-hyperglycemic activity and improves glucose homeostasis by ameliorating β-cell dysfunction in type 2 diabetic mice. It protects β-cells from cytokine- or STZ-induced cell death and restores β-cell function. These in vivo effects support its potential for treating type 2 diabetes and related metabolic disorders.
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| Enzyme Assay |
The in vitro receptor binding/ion channel assay for BBT is not applicable, as the compound acts through cAMP/PKA and Ca2+ channel pathways rather than a specific receptor. Its effects on these pathways can be assessed using cell-based assays measuring cAMP levels, PKA activity, and intracellular calcium levels.
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| Cell Assay |
The in vitro cell-based assay for BBT involves culturing pancreatic β-cells or insulinoma cell lines (e.g., MIN6, INS-1) and treating them with the compound to assess effects on insulin secretion and cell survival. Cells are treated with BBT at various concentrations, and glucose-stimulated insulin secretion is measured by ELISA or radioimmunoassay. cAMP levels are measured using ELISA, and intracellular calcium levels are measured using fluorescent calcium indicators (e.g., Fura-2). Cell viability and protection from cytokine- or STZ-induced cell death are assessed using MTT or CellTiter-Glo assays.
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| Animal Protocol |
In vivo animal studies for BBT are conducted in mouse models of type 2 diabetes. Mice are fed a high-fat diet or treated with STZ to induce diabetes. BBT is administered orally or intraperitoneally at various doses. Blood glucose levels, insulin levels, and glucose tolerance are assessed. Pancreatic tissue is collected for histopathological analysis and assessment of β-cell mass and function. Standard protocols for type 2 diabetes models are employed.
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| ADME/Pharmacokinetics |
BBT has a molecular weight of 386.26 and a molecular formula of C18H12BrNO2S. It is a small molecule enhancer of GSIS with anti-hyperglycemic activity. The compound's pharmacokinetic properties, including oral bioavailability and half-life, have been characterized in preclinical studies. It can be formulated for in vivo administration. Detailed PK parameters are available from preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of BBT has been evaluated in preclinical studies. As an enhancer of GSIS that protects β-cells, its primary safety concerns would relate to hypoglycemia and effects on pancreatic function. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. No significant toxicity has been reported in available literature.
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| Additional Infomation |
BBT is a research compound and has not been approved for clinical use. It is an enhancer of impaired glucose-stimulated insulin secretion (GSIS) with anti-hyperglycemic activity. BBT protects β-cells from cytokine- or STZ-induced cell death and acts through the cAMP/PKA and L-type Ca2+ channel/CaMK2 pathways. It is a valuable tool for studying β-cell function, insulin secretion, and type 2 diabetes.
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| Molecular Formula |
C18H12BRNO2S
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|---|---|
| Molecular Weight |
386.26
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| Exact Mass |
384.98
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| Elemental Analysis |
C, 55.97; H, 3.13; Br, 20.69; N, 3.63; O, 8.28; S, 8.30
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| CAS # |
445000-45-3
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| Appearance |
Light yellow to brown solid powder
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| InChi Key |
FCSCANHTNNHZOH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H12BrNO2S/c19-16-11-10-15(23-16)18(22)20-14-9-5-4-8-13(14)17(21)12-6-2-1-3-7-12/h1-11H,(H,20,22)
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| Chemical Name |
N-(2-benzoylphenyl)-5-bromothiophene-2-carboxamide
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| Synonyms |
BBT
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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 | 2.5889 mL | 12.9446 mL | 25.8893 mL | |
| 5 mM | 0.5178 mL | 2.5889 mL | 5.1779 mL | |
| 10 mM | 0.2589 mL | 1.2945 mL | 2.5889 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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