CAS NO: | 1832576-04-1 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | MLT-943 is a potent, selective and orally activeMALT1proteaseinhibitor. MLT-943 inhibits stimulated-IL-2 secretion in PBMC or in whole blood with a similarIC50 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[1]. | ||||||||||||||||
体外研究 (In Vitro) | MLT-943 shows a high potency and selectivityin vitro. MLT-943 inhibits stimulated IL-2 secretion in PBMC or in whole blood with a similar IC50across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood)[1]. | ||||||||||||||||
体内研究 (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[1].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[1].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[1].MLT-943 (p.o. admistration; 3 mg/kg; single dose) exhibits a good PK parametersin vivo. The Cmaxvalues 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[1].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)[1].
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分子量 | 414.77 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C16H14ClF3N6O2 | ||||||||||||||||
CAS 号 | 1832576-04-1 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(602.74 mM;Need ultrasonic) 配制储备液
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