基本属性 生物活性靶点体外研究体内研究 用途与合成方法 ((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE 价格(试剂级) 供应商 供应信息
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((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

英文名称:Z-FL-COCHO
CAS号:1373215-15-6
分子式:C25H29FN4O5
分子量:484.52
EINECS号:
Mol文件:Mol File
((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE 结构式

((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE 性质

沸点 701.6±60.0 °C(Predicted)
密度 1.38±0.1 g/cm3(Predicted)
储存条件 Store at -20°C
溶解度 DMSO 中≥24.25 mg/mL;不溶于水;不溶于乙醇
形态 粉末
酸度系数(pKa) 12.50±0.46(Predicted)

((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE 用途与合成方法

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.

安全信息

海关编码2934999090

((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE 价格(试剂级)

更新日期 产品编号 产品名称 CAS号 包装 价格
2024-04-30 HY-15533 1 mg 1043
2024-04-30 HY-15533 ((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE 1373215-15-6 2mg 1413

((3R,4S)-4-((4-FLUOROBENZOYL)AMINO)-6-(4-(OXETAN-3-YL)PIPERAZIN-1-YL)CHROMAN-3-YL)N-METHYLCARBAMATE供应商 更多

上海楼岚生物科技有限公司
现货
联系电话:021-52996696,15000506266 15000506266
产品介绍:
英文名称:LY3000328
CAS:1373215-15-6
纯度:>98%
包装信息:2g
备注:2g
库存量:2g
现货日期:2024/6/4 14:47:09
武汉多普乐生物医药有限公司
现货
联系电话:+86-02787215551 +86-19945035818
产品介绍:
英文名称:LY3000328
CAS:1373215-15-6
纯度:99% HPLC
包装信息:10mg;1g;5KG;1KG
库存量:100mg
现货日期:2024/6/17 11:38:31
合肥恩立医药科技有限公司
联系电话:0551-66399836 18955197623
产品介绍:
英文名称:Z-FL-COCHO
CAS:1373215-15-6
纯度:>97%
包装信息:1g,5g,100g,500g,1Kg,10kg
上海喀露蓝科技有限公司
联系电话: 18149758185
产品介绍:
英文名称:LY3000328,Cathepsin S inhibitor
CAS:1373215-15-6
纯度:98%
包装信息:1g;10g;100g
四川省维克奇生物科技有限公司
联系电话:028-81700200 18116577057
产品介绍:
中文名称:暂无
英文名称:LY3000328
CAS:1373215-15-6
纯度:98%
包装信息:5mg;10mg;20mg;50mg;100mg;200mg;500mg;1g

最新发布供应信息

1373215-15-6Cathepsin S inhibitor
上海一研生物科技有限公司 2024-06-12