CAS NO: | 866028-26-4 |
包装 | 价格(元) |
2mg | 电议 |
5mg | 电议 |
25mg | 电议 |
Storage | Store at -20°C |
M.Wt | 224.68 |
Cas No. | 866028-26-4 |
Formula | C12H13ClO2 |
Solubility | ≥22.5 mg/mL in DMSO; ≥41.9 mg/mL in H2O; ≥47.9 mg/mL in EtOH |
Chemical Name | ethyl 2-(2-chlorobenzyl)acrylate |
Canonical SMILES | CCOC(C(CC1=CC=CC=C1Cl)=C)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
INF39 is a nontoxic, irreversible inhibitor of the nucleotide-binding oligomerization domain, leucine-rich repeat and pyrin domain containing protein 3 (NLRP3). NLRP3 is an intracellular sensor that detects a variety of endogenous danger signals, microbial motifs as well as environmental irritants, resulting in the formation and activation of the NLRP3 inflammasome. Assembly of the NLRP3 inflammasome leads to caspase 1-dependent release of pro-inflammatory cytokines (e.g. IL-1β and IL-18), as well as to gasdermin D-induced pyroptotic cell death. Pharmacological inhibition of NLRP3 inflammasome activation has been shown to offer a new option in the treatment of inflammatory bowel disease.
References:
1. Cocco M, Pellegrini C, Martínez-Banaclocha H, et al. Development of an acrylate derivative targeting the NLRP3 inflammasome for the treatment of inflammatory bowel disease. Journal of Medicinal Chemistry, 2017, 60(9): 3656-3671.
2. Swanson KV, Deng M, Ting JP. The NLRP3 inflammasome: molecular activation and regulation to therapeutics. Nature Reviews Immunology, 2019, 19(8): 477-489.
Cell experiment:[1] | |
Cell lines | LPS-primed mouse bone marrow derived macrophages (BMDMs) |
Reaction Conditions | 10 or 100 μM INF39 for 1 h incubation |
Applications | INF39 was able to significantly inhibit ATP- and nigericin-induced IL-1β release at 10 μM. Furthermore, INF39 reduced caspase-1 activation and pyroptosis in these macrophages. |
Animal experiment:[1] | |
Animal models | Male Sprague-Dawley rats, 200 ~ 250 g |
Dosage form | 12.5, 25.0, 50.0 mg/kg Once daily by intragastric route for 6 days |
Applications | Oral administration of INF39 reduced systemic and colonic Inflammation in rats treated with 2,4-dinitrobenzenesulfonic acid (DNBS). Meanwhile, INF39 dose-dependently attenuated increment of spleen weight and decrease in colonic length caused by DNBS. |
Note | The technical data provided above is for reference only. |
References: 1. Cocco M, Pellegrini C, Martínez-Banaclocha H, et al. Development of an acrylate derivative targeting the NLRP3 inflammasome for the treatment of inflammatory bowel disease. Journal of Medicinal Chemistry, 2017, 60(9): 3656-3671. 2. Swanson KV, Deng M, Ting JP. The NLRP3 inflammasome: molecular activation and regulation to therapeutics. Nature Reviews Immunology, 2019, 19(8): 477-489. |