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首页-小分子抑制剂&激动剂-Immunology/Inflammation-NOD-like Receptor (NLR)-OLT1177
OLT1177

Chemical Structure : OLT1177

CAS No.: 54863-37-5

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OLT1177 (Dapansutrile, OLT-1177)

货号: PC-24509Not For Human Use, Lab Use Only.

OLT1177 (Dapansutrile) is an orally active β-sulfonyl nitrile molecule, inhibits activation of the NLRP3 inflammasome, prevents NLRP3-ASC, as well as NLRP3-caspase-1 interaction, thus inhibiting NLRP3 inflammasome oligomerization.

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10 mg ￥580 In stock
25 mg ￥980 In stock
50 mg ￥1480 In stock
100 mg ￥2380 In stock
250 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

OLT1177 (Dapansutrile) is an orally active β-sulfonyl nitrile molecule, inhibits activation of the NLRP3 inflammasome, prevents NLRP3-ASC, as well as NLRP3-caspase-1 interaction, thus inhibiting NLRP3 inflammasome oligomerization.
OLT1177 reduces IL-1β and IL-18 release following canonical and noncanonical NLRP3 inflammasome activation at nanomolar concentrations.
OLT1177 decreased IL-1β levels by 60% and IL-18 by 70% at concentrations 100-fold lower in vitro in LPS-stimulated human blood-derived macrophages.
OLT1177 also reduced IL-1β release and caspase-1 activity in freshly obtained human blood neutrophils.
OLT1177 inhibited LPS-induced IL-1β release by 84% and 36% in monocytes isolated from patients with cryopyrin-associated periodic syndrome (CAPS).
OLT1177 (1 and 10 µM) reduced ATPase activity of recombinant NLRP3.
OLT1177 significantly lowered steady-state levels of phosphorylated NF-κB and IkB kinase in spleen cells from OLT1177-treated mice.

物理化学性质&存储条件

分子量 133.17
分子式 C4H7NO2S
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

3-Methanesulfonylpropanenitrile

参考文献

1. Toldo S, et al. J Cardiovasc Pharmacol. 2019 Apr;73(4):215-222.

2. Marchetti C, et al. Proc Natl Acad Sci U S A. 2018 Feb 13;115(7):E1530-E1539.

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