LasB-IN-3
LasB-IN-3 is a protease elastase (LasB) inhibitor of Pseudomonas aeruginosa with an IC50 value of 8.5 nM. LasB-IN-3 shows an IC50 of 58.9 nM for the Met128Val mutant. LasB-IN-3 binds to active sites of wild-type and Met128Val mutant LasB, coordinates zinc ions, forms hydrogen bonds and CH-π interactions, and inhibits LasB proteolytic activity. LasB-IN-3 increases survival rate in LasB-induced acute lung injury mice models. LasB-IN-3 can be used for the research of Pseudomonas aeruginosa infection.
For research use only. We do not sell to patients.
- CAS No.: 2762675-42-1
- Formula: C18H21ClNO4P
- Molecular Weight:381.79
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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LasB 8.5 nM (IC50) |
LasB-IN-3 (Compound 21) potently inhibits wild-type Pseudomonas aeruginosa LasB with an IC50 of 8.5 ± 0.5 nM, and its activity is reduced ~7-fold against the Met128Val variant (IC50 = 58.9 nM)[1].
LasB-IN-3 inhibits Pseudomonas aeruginosa LasB with an IC50 of 45 nM in the presence of porcine pulmonary surfactant, with reduced activity attributed to 37.2 ± 0.8% binding to surfactant proteins[1].
LasB-IN-3 (0-100 μMM) exhibits minimal cytotoxicity against human A549, HepG2, and HEK293 cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 | C0 | AUC0-t | MRT | Vz | CL_obs |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 2.30 ± 0.4 h | 8.55 ± 6.96 μg/mL | 4.68 ± 1.18 μg/mL·h | 2.8 ± 0.6 h | 1.19 ± 0.4 L/kg | 5.89 ± 1.2 mL/min/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (8-week-old male; acute lung injury model via intranasal instillation of 40 μg purified Pseudomonas aeruginosa LasB elastase)[1]
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Dosage:300 μM
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Administration:intranasal; single dose (preincubated with LasB prior to instillation)
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Result:Achieved 100% survival over 7 days.
Chemical Information
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CAS No. 2762675-42-1
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Molecular Weight 381.79
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Formula C18H21ClNO4P
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SMILES
O=C(NC1=CC=C(C=C1)C2=CC=C(C=C2)Cl)C(CC(C)C)P(O)(O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LasB-IN-3 Related Classifications
HY-181647 Related Classifications
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