计算溶液所需的质量、体积或浓度。
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
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC 50 of 0.04 μM for L. donovani proteasome and an EC 50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research.
In Vitro
LXE408 (compound 1) can occupy the pocket as a ternary complex with the proteasome. LXE408 shows no inhibition of the hERG channel (IC 50 >30 μM) in a manual patch clamp assay. LXE408 has a low propensity to cross the blood brain barrier (brain/plasma AUC ratio=0.03 in mice). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
LXE408 (compound 1; 0.3-10 mg/kg; PO; twice daily for 8 days) potently reduces the parasite burden in the liver in a dose-dependent manner . LXE408 (1, 3, 10, 20 mg/kg; p.o.; b.i.d.; for 10 days) effects robust healing of parasite-induced skin lesions at the base of the tail in BALB/c mice infected with L. major . LXE408 (5 mg/kg IV and 20 mg/kg PO) has a T 1/2 of 3.3 hours for mouse. LXE408 (3 mg/kg IV and 10 mg/kg PO) has a T 1/2 of 3.8 hours, a CL of 2.1 mL/min•kg, and a V ss of 0.53 L/kg for male Sprague-Dawley rat . LXE408 (0.3 mg/kg IV and 1.0 mg/kg PO) has a T 1/2 of 3.8 hours for male beagle dog. LXE408 (0.3 mg/kg IV and 10 mg/kg PO) has a T 1/2 of 9.7 hours for male cynomolgus monkey . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female BALB/c mice (6-8 weeks old) infected with L. donovani Dosage: 0.3, 1, 3, 10 mg/kg Administration: PO; twice daily for 8 days Result: Led to a 95% and >99.84% reduction of parasite burden in the liver at 1 mg/kg and 10 mg/kg. Animal Model: Balb/C mice Dosage: 5 mg/kg IV and 20 mg/kg PO (Pharmacokinetic Analysis) Administration: IV or PO Result: Had a T 1/2 of 3.3 hours, a CL of 2.3 mL/min•kg, and a V ss of 0.63 L/kg for mouse.
规格
规格或纯度
10mM in DMSO
英文名称
LXE408
生化机理
LXE408 是一种口服活性、非竞争性和神经细胞选择性蛋白酶体抑制剂。LXE408 对多诺万病菌蛋白酶体的 IC 50 为 0.04 μM，对多诺万病菌的 EC 50 为 0.04 μM。LXE408 穿过血脑屏障的可能性较低。
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
CC1=C(N=CC=C1)C2=CN3C(=NC(=N3)C4=C(C=CC(=C4)NC(=O)C5=C(N=C(O5)C)C)F)N=C2
关联CAS
PubChem CID
MeSH Entry Terms
LXE408;N-(4-Fluoro-3-(6-(3-methylpyridin-2-yl)-(1,2,4)triazolo(1,5-a)pyrimidin-2-yl)phenyl)-2,4-dimethyl-1,3-oxazole-5-carboxamide
分子量
443.43
技术文档
高级数据
安全和危险性（GHS）
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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