|3-(甲基磺酰基)丙腈|CsnPharm

CAS No.: 54863-37-5

Dapansutrile/3-(甲基磺酰基)丙腈 Catalog No. CSN33194

Synonyms: 3-methanesulfonyl Propanenitrile;OLT1177

OLT1177, a β-sulfonyl nitrile molecule, is a selective inhibitor of the NLRP3 inflammasome, with unique properties to reverse the metabolic costs of inflammation and to treat IL-1β– and IL-18–mediated diseases.

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描述NLRP3 inflammasome can be widely found in epithelial cells and immune cells. The NOD-like receptors (NLRs) family member NLRP3 contains a central nucleotide-binding and oligomerization (NACHT) domain which facilitates self-oligomerization and has ATPase activity^[1]. Dapansutrile（OLT1177） is a potent, selective and orally active inhibitor of NLRP3 inflammasome. Anti-inflammatory, analgesic activity^[2]. OLT1177 specifically inhibited both canonical and noncanonical NLRP3 inflammasome activation in vitro, and showed no effect on the AIM2 and NLRC4 inflammasomes. OLT1177 reduced caspase-1 activity and IL-1β production in monocytes from patients with CAPS and alleviated the severity of LPS-induced systemic inflammation in vivo. Importantly, no biochemical or hematological adverse effects were observed in humans receiving a high concentration of OLT1177 for 8 days. Like CY-09, OLT1177 exerts its anti-inflammatory effect on NLRP3 inflammasome activation independently of signal 1 (NLRP3 and pro-IL-1β expression) or K+ efflux,but directly binds to NLRP3 and inhibits ATPase activity^[3]. In vivo, tumor-associated NLRP3/IL-1 signaling induced expansion of myeloid-derived suppressor cells (MDSCs), leading to reduced natural killer and CD8+ T cell activity concomitant with an increased presence of regulatory T (Treg) cells in the primary tumors. Either genetic or pharmacological inhibition of tumor-derived NLRP3 by dapansutrile (OLT1177) was sufficient to reduce MDSCs expansion and to enhance antitumor immunity, resulting in reduced tumor growth^[4].
参考文献

[1] Yu Zhen, Hu Zhang. NLRP3 Inflammasome and Inflammatory Bowel Disease. Front Immunol. 2019 Feb 28;10:276.
[2] Toldo S, et al. The NLRP3 Inflammasome Inhibitor, Dapansutrile, Reduces Infarct Size and Preserves Contractile Function After Ischemia Reperfusion Injury in the Mouse. J Cardiovasc Pharmacol. 2019 Apr;73(4):215-222.
[3] Marchetti, C. et al. OLT1177, a β-sulfonyl nitrile compound, safe in humans,inhibits the NLRP3 inflammasome and reverses the metabolic cost of inflammation. Proc. Natl. Acad. Sci. USA 115, 89 (2018).
[4] Isak W Tengesdal, Dinoop R Menon,et al. Targeting tumor-derived NLRP3 reduces melanoma progression by limiting MDSCs expansion. Proc Natl Acad Sci U S A. 2021 Mar 9;118(10):e2000915118.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 7.5093 mL
- 37.5463 mL
- 75.0926 mL
- 5 mM
- 1.5019 mL
- 7.5093 mL
- 15.0185 mL
- 10 mM
- 0.7509 mL
- 3.7546 mL
- 7.5093 mL

技术信息

CAS号	54863-37-5	储存条件	粉末 Sealed in dry,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C4H7NO2S	运输	蓝冰
分子量	133.17	别名	3-methanesulfonyl Propanenitrile;OLT1177

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Dapansutrile/3-(甲基磺酰基)丙腈 Catalog No. CSN33194

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