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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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1226697-79-5
- 分子式: C15H14BrN5O3S
- 分子量:424.27
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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PDE4B 160 nM (IC50) |
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.
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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.
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.
化学情報
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CAS 番号 1226697-79-5
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分子量 424.27
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)