计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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.
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 IC 50 across species (0.07-0.09 μM in PBMC, 0.6-0.8 μM in whole blood). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 Foxp 3+ 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) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Naïve rats Dosage: 5 mg/kg Administration: Oral gavage; 5 mg/kg, 10 consecutive days or 0.1 mg/kg MLT-943 Result: Induced a severe immune-mediated pathology after a prolonged treatment
规格
规格或纯度
10mM in DMSO
英文名称
MLT-943
生化机理
MLT-943是一种强效、选择性和口服活性MALT1蛋白酶抑制剂。xa0MLT-943可抑制PBMC或全血中受刺激的IL-2分泌，不同物种的IC50相似（PBMC为0.07-0.09 μM，全血为0.6-0.8 μM）。MLT-943 具有抗流感的作用。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C[C@@H](C1=C(C=NC2=CC(=NN21)Cl)NC(=O)NC3=CC(=NC=C3)C(F)(F)F)OC
PubChem CID
分子量
414.77
技术文档
高级数据
关联靶点（人）
MALT1
Tchem
粘膜相关淋巴组织淋巴瘤易位蛋白1(Mucosa-associated lymphoid tissue lymphoma translocation protein 1)
(3 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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