规格

价格

库存

数量

1 mg

¥ 788

现货

2 mg

¥ 1,170

现货

5 mg

¥ 1,760

现货

10 mg

¥ 2,280

现货

25 mg

¥ 3,890

现货

50 mg

¥ 5,570

现货

100 mg

¥ 7,790

现货

1 mL x 10 mM (in DMSO)

¥ 1,870

现货

生物活性

产品描述	LY 3000328 (Cathepsin S inhibitor) is a selective inhibitor of cathepsin S with IC50 values of 7.7 and 1.67 nM for human and mouse cathepsin S, respectively. LY 3000328 (Cathepsin S inhibitor) may slow or prevent abdominal aortic aneurysm (AAA) expansion and/or reduce the risk of AAA rupture by inhibiting cathepsin S-mediated degradation of extracellular matrix proteins, elastin and collagen.
靶点活性	Cathepsin S (human):7.7 nM, Cathepsin S (mouse):1.67 nM
体外活性	方法：LY 3000328 (Cathepsin S inhibitor)在 hCat S 和 mCat S 酶抑制试验中评估了活性。结果：LY 3000328 (Cathepsin S inhibitor)抑制人和小鼠Cat S 的IC50分别为7.7±5.85和1.67±1.17 nM。[1]
体内活性	方法：研究 LY 3000328 (Cathepsin S inhibitor)（1,3,10,30mg/kg,口服，28天）在BID 小鼠体内的药效。结果：LY 3000328 (Cathepsin S inhibitor)最低剂量为 1 mg/kg 时，主动脉直径减小了58%，3 mg/kg时减小了83%，10 mg/kg时减小了87%；LY 3000328暴露量（AUC）均呈剂量依赖性增加方式，表药物处置性能较好。[1]
别名	Cathepsin S inhibitor

化学信息

分子量	484.52
分子式	C₂₅H₂₉FN₄O₅
CAS No.	1373215-15-6
Smiles	CNC(=O)O[C@H]1COc2ccc(cc2[C@@H]1NC(=O)c1ccc(F)cc1)N1CCN(CC1)C1COC1
密度	1.38 g/cm3 (Predicted)
颜色	White
物理性状	Solid

储存&溶解度

存储

store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 62.5 mg/mL (128.99 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.13 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO