1. Metabolic Enzyme/Protease
  2. Furin
  3. BOS-318

BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furin inhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease.

For research use only. We do not sell to patients.

BOS-318 Chemical Structure

BOS-318 Chemical Structure

CAS No. : 2387633-15-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 151 In-stock
Solution
10 mM * 1 mL in DMSO USD 151 In-stock
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10 mg USD 195 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furin inhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease[1][2].

In Vitro

BOS-318 (0.001-1 μM, 72 hours) provides cytoprotection against toxicity in CuFi-1 cells induced by P aeruginosa exotoxin A (PEA)[1].
BOS-318 (U2OS cells) to be approximately 13 times more potent against furin than PCSK5 (IC50 = 25.3 nM), 24 times more potent than PCSK7 (IC50 = 45.8 nM), and 110 times more potent than PCSK6 (IC50 = 209.4 nM) [1].
BOS-318 (0.3 μM, 2 hours or 48 hours) reduces ENaC-mediated Na+ absorption in CF HBECs and protects against NE- and CF sputum-sol-mediated activation of the ENaC[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: CuFi-1 cells
Concentration: 17.4 and 263.0 nM
Incubation Time: 2 and 48 hours
Result: Significantly inhibited ENaC-mediated Na+ transport as measured in differentiated human bronchial epithelial cells under both short- (IC50= 263.0 nM) and long-term (IC50= 17.4 nM) treatment conditions.

Cell Viability Assay[1]

Cell Line: CuFi-1 cells
Concentration: 0.3 μM
Incubation Time: 72 hours
Result: Significantly increased cell viability in PEA-treated cells to approximately 88% of control levels.

Cell Cytotoxicity Assay[1]

Cell Line: CuFi-1 cells
Concentration: 0.001, 0.01, 0.03, 0.1, 0.3 and 1 μM
Incubation Time: 72 hours
Result: Provided protection against PEA-mediated cytotoxicity in a dose-dependent manner, over a period of 72 h, with an EC50 of 47.8 nM.
Molecular Weight

571.50

Formula

C28H32Cl2N6O3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)CC1CCN(CC2=CC(C3=CC(Cl)=CC(Cl)=C3)=NC(OC4=CN=C(N5CCN(C)CC5)N=C4)=C2)CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (87.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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C2

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V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (4.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7498 mL 8.7489 mL 17.4978 mL 43.7445 mL
5 mM 0.3500 mL 1.7498 mL 3.4996 mL 8.7489 mL
10 mM 0.1750 mL 0.8749 mL 1.7498 mL 4.3745 mL
15 mM 0.1167 mL 0.5833 mL 1.1665 mL 2.9163 mL
20 mM 0.0875 mL 0.4374 mL 0.8749 mL 2.1872 mL
25 mM 0.0700 mL 0.3500 mL 0.6999 mL 1.7498 mL
30 mM 0.0583 mL 0.2916 mL 0.5833 mL 1.4582 mL
40 mM 0.0437 mL 0.2187 mL 0.4374 mL 1.0936 mL
50 mM 0.0350 mL 0.1750 mL 0.3500 mL 0.8749 mL
60 mM 0.0292 mL 0.1458 mL 0.2916 mL 0.7291 mL
80 mM 0.0219 mL 0.1094 mL 0.2187 mL 0.5468 mL
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BOS-318 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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BOS-318
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