LasB-IN-3
Based on 1 Customer Validation
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.
- Purity : 98.81%
- CAS No.: 2762675-42-1
- Formula: C18H21ClNO4P
- Molecular Weight:381.79
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
LasB 8.5 nM (IC50) |
In Vitro
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.
Parmacokinetics
| 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 |
In Vivo
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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Appearance Solid
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Molecular Weight 381.79
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Formula C18H21ClNO4P
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Color Off-white to light brown
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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
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (261.92 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (274 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
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 | 2.6192 mL | 13.0962 mL | 26.1924 mL | 65.4810 mL |
| 5 mM | 0.5238 mL | 2.6192 mL | 5.2385 mL | 13.0962 mL | |
| 10 mM | 0.2619 mL | 1.3096 mL | 2.6192 mL | 6.5481 mL | |
| 15 mM | 0.1746 mL | 0.8731 mL | 1.7462 mL | 4.3654 mL | |
| 20 mM | 0.1310 mL | 0.6548 mL | 1.3096 mL | 3.2741 mL | |
| 25 mM | 0.1048 mL | 0.5238 mL | 1.0477 mL | 2.6192 mL | |
| 30 mM | 0.0873 mL | 0.4365 mL | 0.8731 mL | 2.1827 mL | |
| 40 mM | 0.0655 mL | 0.3274 mL | 0.6548 mL | 1.6370 mL | |
| 50 mM | 0.0524 mL | 0.2619 mL | 0.5238 mL | 1.3096 mL | |
| 60 mM | 0.0437 mL | 0.2183 mL | 0.4365 mL | 1.0914 mL | |
| 80 mM | 0.0327 mL | 0.1637 mL | 0.3274 mL | 0.8185 mL | |
| 100 mM | 0.0262 mL | 0.1310 mL | 0.2619 mL | 0.6548 mL |
LasB-IN-3 Related Classifications
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