| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| ln Vitro |
BOS-318 (0.001–1 μM, 72 hours) offers cytoprotection against CuFi-1 cytotoxicity caused by Pseudomonas aeruginosa exotoxin A (PEA) [1]. The furin-resistance of BOS-318 (U2OS cells) is roughly 13 times more than that of PCSK5 (IC50 = 25.3 nM), 24 times greater than that of PCSK7 (IC50 = 45.8 nM), and 110 times greater than that of PCSK6 (IC50 = 209.4 nM). [1]. NE and CF sputum sol-mediated ENaC activation is inhibited by BOS-318 (0.3 μM, 2 hours or 48 hours) and ENaC-mediated Na+ uptake in CF HBEC is decreased [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: CuFi-1 Cell Tested Concentrations: 17.4 and 263.0 nM Incubation Duration: 2 and 48 hrs (hours) Experimental Results: Significant inhibition of ENaC measured in differentiated human bronchial epithelial cells at two short concentration conditions mediated Na+ transport (IC50= 263.0 nM) and long-term (IC50= 17.4 nM) treatment conditions. Cell viability assay[1] Cell Types: CuFi-1 Cell Tested Concentrations: 0.3 μM Incubation Duration: 72 hrs (hours) Experimental Results: Cell viability in PEA-treated cells increased Dramatically to approximately 88% of control levels. Cytotoxicity assay[1] Cell Types: CuFi-1 Cell Tested Concentrations: 0.001, 0.01, 0.03, 0.1, 0.3 and 1 μM Incubation Duration: 72 hrs (hours) Experimental Results: Provides PEA-mediated cytotoxicity against PEA in a dose-dependent manner over time Toxicity protection for 72 hrs (hours) with EC50 of 47.8 nM. |
| References |
| Molecular Formula |
C28H32CL2N6O3
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|---|---|
| Molecular Weight |
571.50
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| Exact Mass |
570.191
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| CAS # |
2387633-15-8
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| PubChem CID |
146241691
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
39
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| Complexity |
764
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AZEJIKZNBHEXCM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H32Cl2N6O3/c1-34-6-8-36(9-7-34)28-31-16-24(17-32-28)39-26-11-20(18-35-4-2-19(3-5-35)12-27(37)38)10-25(33-26)21-13-22(29)15-23(30)14-21/h10-11,13-17,19H,2-9,12,18H2,1H3,(H,37,38)
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| Chemical Name |
2-[1-[[2-(3,5-dichlorophenyl)-6-[2-(4-methylpiperazin-1-yl)pyrimidin-5-yl]oxypyridin-4-yl]methyl]piperidin-4-yl]acetic acid
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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 : ~50 mg/mL (~87.49 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.37 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 (4.37 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 (4.37 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 | 1.7498 mL | 8.7489 mL | 17.4978 mL | |
| 5 mM | 0.3500 mL | 1.7498 mL | 3.4996 mL | |
| 10 mM | 0.1750 mL | 0.8749 mL | 1.7498 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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