PDE4B-IN-7
PDE4B-IN-7 is a PDE-4B inhibitor with an IC50 of 160 nM. PDE4B-IN-7 can form a firm and stable binding with the active site of PDE-4B. PDE4B-IN-7 inhibits acetylcholine-induced bronchospasm in guinea pigs. PDE4B-IN-7 exerts activity against susceptible Gram-positive and Gram-negative bacterial strains. PDE4B-IN-7 can be used for the researches of asthma and bacterial agent.
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- CAS No.: 1226697-79-5
- Formule: C15H14BrN5O3S
- Masse moléculaire:424.27
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
PDE4B 160 nM (IC50) |
In Vitro
PDE4B-IN-7 (Compound 17k) (1-1000 ng/mL; 20 min) potently inhibits human recombined PDE-4B in vitro with an IC50 of 160 nM[1].
PDE4B-IN-7 (31.15-500 μg/mL; 18-24 h) shows potent in vitro antibacterial activity against S. aureus (MIC = 0.07 μg/mL) and significant activity against E. coli (MIC = 8.074 μg/mL)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:S. aureus and E. coli
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Concentration:31.15–500 μg/mL
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Incubation Time:18-24 h
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Result:Showed a MIC of 0.07 μg/mL for S. aureus and MIC of 8.074 μg/mL for E. coli.
In Vivo
PDE4B-IN-7 (i.p.) has an LD50 of 300 mg/kg via intraperitoneal injection in male albino mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Hartley (male, 300-400 g, bronchospasm induced by acetylcholine injection)[1]
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Dosage:2.5 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.p.
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Result:Reduced acetylcholine-induced bronchospasm by 25.1% at 2.5 mg/kg.
Reduced acetylcholine-induced bronchospasm by 47.9% at 5 mg/kg.
Reduced acetylcholine-induced bronchospasm by 78.3% at 10 mg/kg.
Achieved an IC50 value of 5.8 mg/kg.
Chemical Information
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CAS No. 1226697-79-5
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Masse moléculaire 424.27
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Formule C15H14BrN5O3S
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SMILES
O=C1C2=C(N=C(SCC(NC3=CC=C(Br)C=C3)=O)N2)N(C)C(N1C)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
PDE4B-IN-7 Related Classifications
HY-181770 Related Classifications
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