MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

CAS No. : 1832576-04-1

MCE 国际站：MLT-943

产品活性：MLT-943 是一种有效的、选择性的、口服活性的 MALT1 protease 抑制剂。MLT-943 可抑制 PBMC 或全血中 IL-2 的分泌，PBMC 中抑制的 IC₅₀ 值为 0.07~0.09 μM，全血中抑制的 IC₅₀ 值为 0.6~0.8 μM)。MLT-943具有抗炎活性，可用于 FcgR 介导的炎症研究。

研究领域：Metabolic Enzyme/Protease  |  NF-κB

作用靶点：MALT1

In Vitro: MLT-943 shows a high potency and selectivity in vitro. MLT-943 inhibits stimulated IL-2 secretion in PBMC or in whole blood with a similar IC₅₀ across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood).

In Vivo: MLT-943 (oral gavage; 10 mg/kg; QD) prophylactic treatment in the rat collagen-induced arthritis model suppresses anti-collagen antibody production, fully prevents paw swelling, and normalizes joint histology scores in rat model.
MLT-943 (oral gavage; 5 mg/kg; QD; 10 consecutive days) effectively inhibits MALT1 protease activity and results in a progressive reduction in the frequency of Foxp³⁺CD25⁺ Treg cells in circulating CD4⁺ T cells, which was maximal after 7 days of treatment. And Discontinuation of MLT-943 treatment after day 10 leads to Treg frequency progressively returning to their original values within 4 days. Suboptimal doses of MLT-943 (0.1 and 0.5 mg/kg QD; p.o.) does not impact the Treg frequency.
MLT-943 (oral gavage; 0, 5, 20 or 80 mg/kg/day; 4-13 weeks) causes a reduction in Treg and an increase in total T cell counts, in both 4- and 13-week rat toxicity studies at all dose levels. While a 4-Longer treatment induces severe immune-mediated pathology in multiple organs, with clinical onset starting around week 9 in rat.
MLT-943 (p.o. admistration; 3 mg/kg; single dose) exhibits a good PK parameters in vivo. The C_max values are 0.7 nM and 0.5 nM, respectively in rat and mice, respectively. And the F% are 86% and 50% in rat and mice, respective.
For i.v. admistration the compound is formed in NMP:PEG200 (30/70); For p.o. admistration solution is formed in MC:Tween 80:Water (0.5:0.5:99) solution (Sourced from literature, for reference only).

相关产品：Mepazine hydrochloride

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供最新最全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。