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CAS No. : 1832576-04-1

MCE 國(guó)際站：MLT-943

產(chǎn)品活性：MLT-943 是一種有效的、選擇性的、口服活性的 MALT1 protease 抑制劑。MLT-943 可抑制 PBMC 或全血中 IL-2 的分泌，PBMC 中抑制的 IC₅₀ 值為 0.07~0.09 μM，全血中抑制的 IC₅₀ 值為 0.6~0.8 μM)。MLT-943具有抗炎活性，可用于 FcgR 介導(dǎo)的炎癥研究。

研究領(lǐng)域：Metabolic Enzyme/Protease  |  NF-κB

作用靶點(diǎn)：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).

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