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首页-小分子抑制剂&激动剂-NF-κB Pathway-NF-κB-AS2690168 free base
AS2690168 free base

Chemical Structure : AS2690168 free base

CAS No.: 1393999-78-4

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AS2690168 free base (AS 2690168)

货号: PC-73379Not For Human Use, Lab Use Only.

AS2690168 is a novel orally available, selective RANKL signal transduction inhibitor, reduces TRAP staining of sRANKL-stimulated RAW264 cells with IC50 of 0.28 uM, suppresses RANKL-induced osteoclastogenesis.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

AS2690168 is a novel orally available, selective RANKL signal transduction inhibitor, reduces TRAP staining of sRANKL-stimulated RAW264 cells with IC50 of 0.28 uM, suppresses RANKL-induced osteoclastogenesis.
AS2690168 suppressed soluble RANKL (sRANKL)-induced NFATc1 mRNA expression in RAW264 cells with 37.1% and 98.9% inhibiyion at 0.3 and 3.0 uM, respectively.
AS2690168 also suppressed calcium release from parathyroid hormone-stimulated mouse calvaria with an IC50 value of 0.46 uM.
AS2690168 (3 mg/kg, p.o.) completely suppressed the decrease in femoral bone mineral content in an sRANKL-induced osteopenic mice model, also significantly suppressed the decrease in femoral bone mineral density and increase in serum tartrate-resistant acid phosphatase-5b levels in ovariectomized rats at doses of 0.3, 1 and 3 mg/kg.
AS260168 suppressed the increase in urine deoxypyridinoline in a rat prednisolone-induced osteoporosis model at 10 mg/kg.

物理化学性质&存储条件

分子量 346.31
分子式 C17H13F3N4O
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

参考文献

1. Morikawa N, et al. Eur J Pharmacol. 2022 Apr 6:174941.

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