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首页-小分子抑制剂&激动剂-NF-κB Pathway-NF-κB-sRANKL inhibitor S3-15
sRANKL inhibitor S3-15

Chemical Structure : sRANKL inhibitor S3-15

CAS No.: 2412947-15-8

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sRANKL inhibitor S3-15 (S3-15)

货号: PC-49334Not For Human Use, Lab Use Only.

sRANKL inhibitor S3-15 is a highly potent, orally active inhibitor of soluble RANKL, selectively interrupt soluble RANKL-RANK interaction and without interfering with the membrane RANKL-RANK interaction, shows potent osteoclast inhibition effect with IC50 of 0.19 uM in vitro.

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5 mg ￥2980 In stock
10 mg ￥4580 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

sRANKL inhibitor S3-15 is a highly potent, orally active inhibitor of soluble RANKL, selectively interrupt soluble RANKL-RANK interaction and without interfering with the membrane RANKL-RANK interaction, shows potent osteoclast inhibition effect with IC50 of 0.19 uM in vitro.
S3-15 can bind to sRANKL at the enlarged stable region (binding site), and unable to bind to mRANKL at the shrunken stable region.
S3-15 inhibits sRANKL induced osteoclast differentiation, while exhibits weak osteoclast differentiation in mRANKL induced osteoclastogenesis assay.
S3-15 suppresses RANKL-induced NF-κB signaling by decreasing the phosphorylation of the IκB kinase-α (IKKα), NF-κB inhibitor-α (IκBα) and p65.
S3-15 dose-dependently blocked both downstream transcription factor NF-κB and NFATC luciferase reporter-gene expression of RANKL-RANK signaling.
S3-15 selectively inhibits sRANKL without changing T lymphocyte differentiation.
S3-15 exhibits anti-osteoporotic effects without causing immunosuppression in ovariectomy (OVX) rats.

物理化学性质&存储条件

分子量 326.312
分子式 C16H14N4O4
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

2-[2-[2-Oxo-1-[(2-pyridinylamino)carbonyl]propylidene]hydrazinyl]benzoic acid

参考文献

1. Huang D, et al. Nat Commun. 2022 Sep 12;13(1):5338.

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