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| 25mg |
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BC-1215 is an inhibitor of F-box protein 3 (FBXO3, a ubiquitin E3 ligase component, IC50=0.9 μg/mL for IL-1β release). BC-1215 decreases Fbxo3-Fbxl2 interaction and prevents SCFFbxo3 catalyzed Fbxl2 ubiquitination. BC-1215 inhibits the Fbxo3-TRAF activation pathway by destabilizing TRAF1–TRAF6. BC-1215, interacts with ApaG to profoundly inhibit secretion of a broad spectrum of TH1 panel cytokines from human PBMC.
| ln Vitro |
By destabilizing TRAF1-6, BC-1215 (0, 0.4, 2, 10, 50 μg/mL; 16 h, 18 h, and 24 h) inhibits the Fbxo3-TRAF activation pathway[1].
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| ln Vivo |
Induced inflammation caused by bacteria is lessened by BC-1215 (i.p.; 100 μg)[1].
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| Animal Protocol |
Animal Model: Sepsis model caused by cecal ligation and puncture (CLP)[1]
Dosage: 100 μg
Administration: i.p.
Result:reduced the number of bacteria in the CLP model and significantly attenuated the release of all three of the circulating pro-inflammatory cytokines when exposed to CLP.
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| References |
| Molecular Formula |
C26H26N4
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|---|---|
| Molecular Weight |
394.51
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| Exact Mass |
394.215
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| CAS # |
1507370-20-8
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| PubChem CID |
72201045
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
589.9±50.0 °C at 760 mmHg
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| Flash Point |
310.6±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.613
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| LogP |
3.68
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
30
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| Complexity |
412
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IXEPQJQQSLMESJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C26H26N4/c1-3-15-29-25(5-1)23-11-7-21(8-12-23)19-27-17-18-28-20-22-9-13-24(14-10-22)26-6-2-4-16-30-26/h1-16,27-28H,17-20H2
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| Chemical Name |
N,N'-bis[(4-pyridin-2-ylphenyl)methyl]ethane-1,2-diamine
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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 : 12.5~79 mg/mL ( 31.68~200.24 )
Ethanol : ~79 mg/mL |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.17 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 12.5 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: ≥ 1.25 mg/mL (3.17 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 12.5 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: ≥ 1.25 mg/mL (3.17 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 | 2.5348 mL | 12.6739 mL | 25.3479 mL | |
| 5 mM | 0.5070 mL | 2.5348 mL | 5.0696 mL | |
| 10 mM | 0.2535 mL | 1.2674 mL | 2.5348 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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