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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Aldose Reductase-ASP9521
ASP9521

Chemical Structure : ASP9521

CAS No.: 1126084-37-4

ASP9521 (ASP 9521;ASP-9521)

货号: PC-60998Not For Human Use, Lab Use Only.

ASP9521(ASP-9521) is a potent, selective, orally bioavailable inhibitor of Aldo-keto reductase 1C3 (17βHSD5, AKR1C3) with IC50 of 11 nM and 49 nM for recombinant human or cynomolgus monkey AKR1C3, respectively.

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25 mg ¥1480 In stock
50 mg ¥2380 In stock
100 mg ¥3980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ASP9521 (ASP-9521) is a potent, selective, orally bioavailable inhibitor of Aldo-keto reductase 1C3 (17βHSD5, AKR1C3) with IC50 of 11 nM and 49 nM for recombinant human or cynomolgus monkey AKR1C3, respectively.
ASP9521 displays >100-fold selectivity for AKR1C3 over the isoform AKR1C2, and does not inhibits AKR1C1 and AKR1C6.
ASP9521 inhibits both aandrostenedione (10 nM)-induced PSA production and cell proliferation in LNCaPAKR1C3 cells with IC50 of 11 nM and 6.6 nM, respectively.
ASP9521 inhibits AD-induced intratumoural T production in CWR22R xenografts.

物理化学性质&存储条件

分子量 330.428
分子式 C19H26N2O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-{1-[(5-methoxy-1H-indol-2-yl)carbonyl]piperidin-4-yl}-2-methylpropan-2-ol

参考文献

1. Loriot Y, et al. Invest New Drugs. 2014 Oct;32(5):995-1004.

2. Kikuchi A, et al. Invest New Drugs. 2014 Oct;32(5):860-70.

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