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。

MLT-943 is a potent, selective and orally active MALT1 protease inhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similar IC 50  across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MLT-943 has anti-inflammatory activities and can be used for FcgR-mediated inflammation research.

Solid

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).
has not independently confirmed the accuracy of these methods. They are for reference only.

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 FoxpCD25 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

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Powder -20°C 3 years；In solvent -80°C 6 months

[1]. Kea Martin, et al. Pharmacological Inhibition of MALT1 Protease Leads to a Progressive IPEX-Like Pathology. Front Immunol
[2]. Jean Quancard, et al. Optimization of the In Vivo Potency of Pyrazolopyrimidine MALT1 Protease Inhibitors by Reducing Metabolism and Increasing Potency in Whole Blood. J Med Chem. 2020 Dec 10;63(23):14594-14608.

In Vitro: DMSO : 250 mg/mL (602.74 mM; Need ultrasonic)配制储备液