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Cathepsin S inhibitor Sale

(Synonyms: LY 3000328) 目录号 : GC14903

A potent cathepsin S inhibitor

Cathepsin S inhibitor Chemical Structure

Cas No.:1373215-15-6

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,309.00
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1mg
¥552.00
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2mg
¥819.00
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5mg
¥1,232.00
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10mg
¥1,596.00
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50mg
¥3,899.00
现货
100mg
¥5,453.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

Kinase assays

Assays were performed for Cat S, mCat S, Cat B and Cat L by adding enzyme to a concentration of FRET substrate equal to the Km in a 50 mM sodium phosphate buffer (pH 6.5) containing 2.5 mM DTT, 2.5 mM EDTA plus 0.01% Triton X-100. The Cat V and Cat K assays were performed as above, but in a 0.1 M sodium acetate (pH 5.5) buffer containing 2.5 mM DTT, 2.5 mM EDTA plus 0.01% Triton X-100. Km values for the FRET substrate were 25 μM, 25 μM, 20 μM, 37.5 μM, 35 μM, 35 μM and 25 μM for human Cat S, mouse Cat S, human Cat L, human Cat B, human Cat K, human Cat V and human Cat F respectively.

Animal experiment [1]:

Animal models

Mouse model of abdominal aortic aneurysm (AAA)

Dosage form

1, 3, 10, and 30 mg/kg, oral, BID dosing

Application

The efficacies of Cathepsin S inhibitor was studied in a mouse model of abdominal aortic aneurysm (AAA). Cathepsin S inhibitor exhibited a dose-responsive aortic diameter reduction at 1, 3, 10, and 30 mg/kg. At the lowest dose of 1 mg/kg of Cathepsin S inhibitor, the aortic diameter is reduced by 58%, then 83% at 3 mg/kg, and 87% at 10 mg/kg.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[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.

产品描述

Ki: 0.185 nM

Cathepsin S is a lysosomal cysteine protease, playing an important role in antigen presentation. The inhibition of Cathepsin S is expected to result in immunosuppression, which makes this enzyme an attractive target to potentially treat autoimmune and inflammatory diseases. Cathepsin S inhibitor is a novel Cathepsin S inhibitor.

In vitro: Cathepsin S inhibitor was a slow, tight-binding reversible inhibitor of recombinant cathepsin S, exhibiting greater selectivity for cathepsin S compared to cathepsin B [1].

In vivo: No animal in vivo data available currently

Clinical trial: Oral Cathepsin S inhibitor that blocked MHCII antigen presentation could result in a T-cell-selective immunosuppressant agent with improved safety over the current standard of care for the treatment of rheumatoid arthritis, psoriasis, multiple sclerosis and other autoimmune-based inflammatory diseases [2].

References:
[1] Wiener JJ, Sun S, Thurmond RL.  Recent advances in the design of cathepsin S inhibitors. Curr Top Med Chem. 2010;10(7):717-32.
[2] Lee-Dutra A, Wiener DK, Sun S.  Cathepsin S inhibitors: 2004-2010. Expert Opin Ther Pat. 2011;21(3):311-37.

Chemical Properties

Cas No. 1373215-15-6 SDF
别名 LY 3000328
化学名 [(3R,4S)-4-[(4-fluorobenzoyl)amino]-6-[4-(oxetan-3-yl)piperazin-1-yl]-3,4-dihydro-2H-chromen-3-yl] N-methylcarbamate
Canonical SMILES CNC(=O)OC1COC2=C(C1NC(=O)C3=CC=C(C=C3)F)C=C(C=C2)N4CCN(CC4)C5COC5
分子式 C25H29FN4O5 分子量 484.52
溶解度 ≥ 24.25 mg/mL in DMSO 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0639 mL 10.3195 mL 20.639 mL
5 mM 0.4128 mL 2.0639 mL 4.1278 mL
10 mM 0.2064 mL 1.0319 mL 2.0639 mL
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