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
提供 ≥99% 纯度，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
-20°C储存。超低温运输 。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
Form:Solid
规格
规格或纯度
≥99%
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
-20°C储存
运输条件
超低温运输
作用类型
抑制剂
纯度
≥99%
名称和识别符
分子类型
未知
IUPAC Name
1-[2-chloro-7-[(1S)-1-methoxyethyl]pyrazolo[1,5-a]pyrimidin-6-yl]-3-[2-(trifluoromethyl)pyridin-4-yl]urea
INCHI
1S/C16H14ClF3N6O2/c1-8(28-2)14-10(7-22-13-6-12(17)25-26(13)14)24-15(27)23-9-3-4-21-11(5-9)16(18,19)20/h3-8H,1-2H3,(H2,21,23,24,27)/t8-/m0/s1
InChi Key
ZMPUACZRXUZAJD-QMMMGPOBSA-N
Smiles
CC(C1=C(C=NC2=CC(=NN21)Cl)NC(=O)NC3=CC(=NC=C3)C(F)(F)F)OC
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
三维结构
交互式化学结构模型
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)
CYP2D6
Tclin
Cytochrome P450 2D6
(33882 活性数据)
CYP2C9
Tchem
Cytochrome P450 2C9
(32119 活性数据)
CYP3A4
Tclin
Cytochrome P450 3A4
(53859 活性数据)
作用机制
| 作用机制 | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | 参考文献 |
|---|
化学和物理性质
溶解性
DMSO : 250 mg/mL (602.74 mM; Need ultrasonic)
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
常见问题
本产品的纯度是多少？
本产品的化学纯度（含量）为 ≥99%。批次的具体数值以分析证书（COA）为准。
本产品应如何储存？
请于?20 °C条件下保存。需冷冻保存以维持规定的有效期。
本产品如何运输？
本产品采用保温箱配冰袋运输。收货后请立即拆包，并按上述储存条件保存。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 1832576-04-1，分子式为 C16H14ClF3N6O2，分子量为 414.77 g/mol。InChIKey ZMPUACZRXUZAJD-QMMMGPOBSA-N。
如何获取批次专用COA？
每个订单都会随附分析证书（COA），您也可以从账户订单历史中下载。如需订购前的COA，请联系您的客户代表，或使用PDP上的"申请COA"按钮——我们将提供代表性批次的COA。
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）