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Synonyms:
LasB-IN-3
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | LasB-IN-3 is an inhibitor of the elastase (LasB) in Pseudomonas aeruginosa, with an IC50 of 8.5 nM. It shows an IC50 of 58.9 nM against the Met128Val mutant. LasB-IN-3 binds to the active sites of both the wild-type and Met128Val mutant LasB, chelating zinc ions and forming hydrogen bonds and CH-π interactions, thus inhibiting the proteolytic activity of LasB. Additionally, LasB-IN-3 enhances the survival rate in a mouse model of acute lung injury induced by LasB. This compound is applicable for studies related to Pseudomonas aeruginosa infections. |
| In vitro | LasB-IN-3 (Compound 21) is a potent inhibitor of wild-type Pseudomonas aeruginosa LasB, with an IC50 of 8.5 ± 0.5 nM, though its activity decreases approximately 7-fold against the Met128Val mutant (IC50 = 58.9 nM). The compound demonstrates an IC50 of 45 nM in the presence of porcine pulmonary surfactant, with reduced activity attributed to a 37.2 ± 0.8% binding rate to surfactant proteins. LasB-IN-3 (0-100 μM) exhibits very low cytotoxicity towards human A549, HepG2, and HEK293 cell lines. |
| In vivo | LasB-IN-3 (Compound 21) (300 μM; intranasal instillation ) achieves a 100% survival rate in C57BL/6 mice with acute lung injury induced by LasB. |
| Molecular Weight | 381.79 |
| Formula | C18H21ClNO4P |
| Cas No. | 2762675-42-1 |
| Smiles | O=C(NC1=CC=C(C=C1)C=2C=CC(Cl)=CC2)C(CC(C)C)P(=O)(O)O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
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