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Aldumastat
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Aldumastat图片
CAS NO:1957278-93-1
包装与价格:
包装价格(元)
5mg电议
10mg电议

产品介绍
Aldumastat (GLPG1972;S201086) 是一种强效、选择性、口服活性 ADAMTS-5 (IC50=19 nM) 抑制剂,其选择性是 ADAMTS-4 (IC50=156 nM) 的 8 倍。Aldumastat 具有抗代谢活性,用于骨关节炎研究。
Cas No.1957278-93-1
别名GLPG1972; S201086
分子式C20H24F2N4O3
分子量406.43
溶解度DMSO : 100 mg/mL (246.04 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Aldumastat (GLPG1972; S201086) is a potent, seletive and orally active ADAMTS-5 (IC50=19 nM) inhibitor, and has 8-fold seletivity over ADAMTS-4 (IC50=156 nM). Aldumastat has anticatabolic activity and is used for osteoarthritis research[1].

GLPG1972 (oral gavage; 5 mg/kg; single dose) displays a favorable PK profile in mice, rats, and dogs. The oral availability (F%) for mice, rats, and dogs are 25%, 58% and 97%, respectively[1].

[1]. Franck Brebion, et al. Discovery of GLPG1972/S201086, a Potent, Selective, and Orally Bioavailable ADAMTS-5 Inhibitor for the Treatment of Osteoarthritis. J Med Chem. 2021 Mar 25;64(6):2937-2952.