貨號	規格	價格	上海	北京	武漢	南京	購買數量
S83028-5mg	≥98%	￥1760.00 S83028-5mg ￥1760.00 2-3天	0 貨期：2-3天	-	-	-
S83028-10mg	≥98%	￥2250.00 S83028-10mg ￥2250.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

LY 3000328 (Z-FL-COCHO) is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.

產品描述：

LY 3000328 (Z-FL-COCHO) is a potent and selective Cathepsin S (Cat S) inhibitor with IC50s of 7.7 and 1.67 nM for hCat S and mCat S, respectively.

靶點：

cathepsin S;CysteineProtease

體外研究：

LY 3000328 maintains excellent in vitro potency and selectivity. LY 3000328 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 LY 3000328 there is only 6% displacement of [3H]-astemizole in an assay with HEK293 membrane preparation, indicating low potential of hERG blockade. LY 3000328 is a potent and specific inhibitor of cathepsin S (CatS). Inhibition of CatS activity in plasma would be 50% of maximal when LY 3000328 plasma concentration is approximately 60 ng/mL

體內研究：

The efficacies of LY 3000328 is studied in a mouse model of abdominal aortic aneurysm (AAA). In this model, inflammation is induced using CaCl2 applied to the ablumenal surface. It is shown that features of the disease state in this model resemble those of human AAA. LY 3000328 exhibits a dose-responsive aortic diameter reduction at 1, 3, 10, and 30 mg/kg. At the lowest dose of 1 mg/kg of LY 3000328, 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 LY 3000328 are favorable

參考文獻：

1. Jadhav PK, et al. Discovery of Cathepsin S Inhibitor LY3000328 for the Treatment of Abdominal Aortic Aneurysm. ACS Med Chem Lett. 2014 Aug 27;5(10):1138-42. 2. Payne CD, et al. Pharmacokinetics and pharmacodynamics of the cathepsin S inhibitor, LY3000328, in healthy subjects. Br J Clin Pharmacol. 2014 Dec;78(6):1334-42.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.064 ml	10.319 ml	20.639 ml
5 mM	0.413 ml	2.064 ml	4.128 ml
10 mM	0.206 ml	1.032 ml	2.064 ml
50 mM	0.041 ml	0.206 ml	0.413 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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