网站主页 >> CAS数据库列表 >> ((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE
((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE
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- CAS号:
- 1373215-15-6
- 英文名:
- Z-FL-COCHO
- 英文别名:
- Z-FL-COCHO;LY 3000328;CATHEPSIN S INHIBITOR;LY3000328，Cathepsin S inhibitor;CATHEPSIN S INHIBITOR ;LY-3000328;LY3000328;Cathepsin,LY3000328,LY 3000328,Inhibitor,LY-3000328,inhibit;(3R,4S)-4-(4-fluorobenzamido)-6-(4-(oxetan-3-yl)piperazin-1-yl)chroman-3-yl methylcarbamate;((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE;N-[(3R,4S)-3,4-Dihydro-3-[[(methylamino)carbonyl]oxy]-6-[4-(3-oxetanyl)-1-piperazinyl]-2H-1-benzopyran-4-yl]-4-fluorobenzamide;Benzamide, N-[(3R,4S)-3,4-dihydro-3-[[(methylamino)carbonyl]oxy]-6-[4-(3-oxetanyl)-1-piperazinyl]-2H-1-benzopyran-4-yl]-4-fluoro-
- 中文名:
- ((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE
- 中文别名:
- LY3000328游离态;化合物LY 3000328;N-[(3R,4S)-3,4-二氢-3-[[(甲基氨基)羰基]氧基]-6-[4-(3-氧杂环丁基)-1-哌嗪基]-2H-1-苯并吡喃-4-基]-4-氟-苯甲酰胺
- CBNumber:
- CB5175767
- 分子式:
- C25H29FN4O5
- 分子量:
- 484.52
- MOL File:
- Mol file
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((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE化学性质
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沸点:
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701.6±60.0 °C(Predicted)
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密度:
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1.38±0.1 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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≥24.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
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形态:
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Powder
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酸度系数(pKa):
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12.50±0.46(Predicted)
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((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE性质、用途与生产工艺
LY 3000328 是一种有效，选择性的 Cathepsin S (Cat S) 抑制剂，抑制人和小鼠Cat S的 IC50 分别为7.7，1.67 nM。
IC50: 7.7±5.85 nM (hCat S), 1.67±1.17 (mCat S)
LY3000328 maintains excellent in vitro potency and selectivity. LY3000328 shows low in vitro CYP450 inhibition (<15% at 10 μM for CYP3A4, CYP2D6, and CYP2C9); low in vitro metabolism in mouse, rat, dog, and human liver microsomes (<20% after 30 min incubation at 4 μM); and good permeability (MDCK A-B>4%). At a 100 μM concentration of LY3000328 there is only 6% displacement of [
3
H]-astemizole in an assay with HEK293 membrane preparation, indicating low potential of hERG blockade. LY3000328 is a potent and specific inhibitor of cathepsin S (CatS). Inhibition of CatS activity in plasma would be 50% of maximal when LY3000328 plasma concentration is approximately 60 ng/mL.
The efficacies of LY3000328 is studied in a mouse model of abdominal aortic aneurysm (AAA). In this model, inflammation is induced using CaCl
2
applied to the ablumenal surface. It is shown that features of the disease state in this model resemble those of human AAA. LY3000328 exhibits a dose-responsive aortic diameter reduction at 1, 3, 10, and 30 mg/kg. At the lowest dose of 1 mg/kg of LY3000328, the aortic diameter is reduced by 58%, then 83% at 3 mg/kg, and 87% at 10 mg/kg. The exposure (AUC) for both compounds increased in a dose-dependent manner, suggesting that the drug disposition properties of LY3000328 are favorable.
((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-15533 | LY 3000328 | | 1 mg | 1043元 |
| 2024/04/30 | HY-15533 | ((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE
LY 3000328 | 1373215-15-6 | 2mg | 1413元 |
((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE
生产厂家
1373215-15-6, ((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE 相关搜索:
- 抑制剂
- C25H29FN4O5
- 化合物LY 3000328
- LY3000328游离态
- N-[(3R,4S)-3,4-二氢-3-[[(甲基氨基)羰基]氧基]-6-[4-(3-氧杂环丁基)-1-哌嗪基]-2H-1-苯并吡喃-4-基]-4-氟-苯甲酰胺
- 1373215-15-6
- Cathepsin,LY3000328,LY 3000328,Inhibitor,LY-3000328,inhibit
- LY3000328，Cathepsin S inhibitor
- CATHEPSIN S INHIBITOR ;LY-3000328;LY3000328
- (3R,4S)-4-(4-fluorobenzamido)-6-(4-(oxetan-3-yl)piperazin-1-yl)chroman-3-yl methylcarbamate
- Benzamide, N-[(3R,4S)-3,4-dihydro-3-[[(methylamino)carbonyl]oxy]-6-[4-(3-oxetanyl)-1-piperazinyl]-2H-1-benzopyran-4-yl]-4-fluoro-
- LY 3000328
- N-[(3R,4S)-3,4-Dihydro-3-[[(methylamino)carbonyl]oxy]-6-[4-(3-oxetanyl)-1-piperazinyl]-2H-1-benzopyran-4-yl]-4-fluorobenzamide
- CATHEPSIN S INHIBITOR
- ((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE
- Z-FL-COCHO