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MLT-943
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MLT-943图片
CAS NO:1832576-04-1
包装与价格:
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

产品介绍
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。
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].

Animal Model:Naive rats[1]
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
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
Powder-20°C3 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 250 mg/mL(602.74 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.4110 mL12.0549 mL24.1097 mL
5 mM0.4822 mL2.4110 mL4.8219 mL
10 mM0.2411 mL1.2055 mL2.4110 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.01 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (5.01 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.01 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。