Verducatib
Based on 1 Customer Validation
Verducatib (BI 1291583) is an orally active inhibitor of cathepsin C (also known as DPP1). Verducatib restores the protease-inhibitor balance by inhibiting the activation of neutrophil serine proteases, thereby alleviating pulmonary inflammation and regulating infection responses. Verducatib significantly reduces the risk (including severe exacerbations) and frequency of acute exacerbations in bronchiectasis (BE). Verducatib also improves lung function and quality of life, and shortens the duration of antibiotic use. The overall incidence of adverse events of Verducatib is comparable to that of placebo, with only slightly more mild-to-moderate cutaneous adverse events observed in the high-dose group, demonstrating promising clinical application potential.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 純度: 98.95%
- CAS 番号: 1887236-33-0
- 分子式: C31H35FN4O3
- 分子量:530.63
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
Cathepsin アイソフォーム固有の製品をすべて表示
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生物活性
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DPP-1 |
Cathepsin C |
Verducatib (BI 1291583) (0.08, 0.4, 2, 10, 50 nM, pH 4.5) binds to recombinant human cathepsin C (CatC) in a reversible covalent manner, with binding kinetic parameters of kon 6.36×106 M-1s-1, koff 2.29×10-3 s-1, an equilibrium dissociation constant KD of 0.43 nM, and a binding half-life t1/2 of 5.19 min[3].
Verducatib (0.064-1000 nM; 48 h) concentration-dependently inhibits the production of active neutrophil elastase (NE) in human neutrophil progenitor U937 cells, with an IC50 of 0.7 nM. It shows no obvious cytotoxicity against U937 cells, with cell viability higher than 93% at all tested concentrations and an average cell viability of 98% at the highest concentration of 1000 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human neutrophil progenitor U937 cells
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Concentration:0.064, 0.32, 1.6, 8, 40, 200, 1000 nM
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Incubation Time:48 h
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Result:Inhibited the production of active neutrophil elastase (NE) in human neutrophil progenitor U937 cells, with an IC50 of 0.7 nM.
Verducatib (single dose; p.o.) exhibits rapid distribution to the target tissue bone marrow and slow clearance in the pharmacokinetic models of healthy mice and rats. Even at low doses, it achieves a distribution profile where bone marrow exposure is significantly higher than plasma exposure, and this property shows no obvious interspecies difference between the two species[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female Crl:NMRI mice, LPS-challenged lung neutrophil influx model for bronchiectasis preclinical mechanism verification[3]
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Dosage:0.005 mg/kg, 0.05 mg/kg, 0.5 mg/kg, 5 mg/kg
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Administration:oral gavage twice daily on Days 1-5, 8 and 9, with final dose on Day 10 followed by nebulised E. coli LPS challenge
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Result:Inhibited the production of active neutrophil elastase (NE) and cathepsin G (CatG) in bronchoalveolar lavage fluid (BALF) neutrophils in a dose-dependent manner.
The maximum inhibition rate of NE reached 97%, with an ED99 value of 1.5 mg/kg for NE inhibition, and the maximum inhibition rate of CatG reached 99%.
Showed statistically significant inhibition of NE activity compared with the vehicle control (p<0.001).
At 5 h after the final dose of 0.5 mg/kg, the mean exposure of BI 1291583 in bone marrow was 2981.7 nM, while the corresponding plasma exposure was 32.5 nM.
化学情報
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CAS 番号 1887236-33-0
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性状 Solid
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分子量 530.63
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分子式 C31H35FN4O3
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Color White to off-white
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SMILES
FC1=C(C[C@@H](C#N)NC([C@@H]2[C@]3([H])C[C@](CC3)([H])N2)=O)C=CC(C4=CC=C5COC6(CCN(C7COC7)CC6)C5=C4)=C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 50 mg/mL (94.23 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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (278 KB)
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SDS (252 KB)
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- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
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 | 1.8846 mL | 9.4228 mL | 18.8455 mL | 47.1138 mL |
| 5 mM | 0.3769 mL | 1.8846 mL | 3.7691 mL | 9.4228 mL | |
| 10 mM | 0.1885 mL | 0.9423 mL | 1.8846 mL | 4.7114 mL | |
| 15 mM | 0.1256 mL | 0.6282 mL | 1.2564 mL | 3.1409 mL | |
| 20 mM | 0.0942 mL | 0.4711 mL | 0.9423 mL | 2.3557 mL | |
| 25 mM | 0.0754 mL | 0.3769 mL | 0.7538 mL | 1.8846 mL | |
| 30 mM | 0.0628 mL | 0.3141 mL | 0.6282 mL | 1.5705 mL | |
| 40 mM | 0.0471 mL | 0.2356 mL | 0.4711 mL | 1.1778 mL | |
| 50 mM | 0.0377 mL | 0.1885 mL | 0.3769 mL | 0.9423 mL | |
| 60 mM | 0.0314 mL | 0.1570 mL | 0.3141 mL | 0.7852 mL | |
| 80 mM | 0.0236 mL | 0.1178 mL | 0.2356 mL | 0.5889 mL |
Verducatib 関連分類
HY-172242 関連分類
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