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LML134 Sale

目录号 : GC38450

LML134 (化合物 18b) 是一种具有口服活性,高选择性 H3R (组胺 3 受体) 反向激动剂,对 hH3R 的 cAMP 和 bdg 的 Kis 分别为 0.3 nM 和 12 nM。LML134 快速穿透大脑,导致高 H3R 占有率,并以快速的动力学特征使其目标脱离。LML134 用于治疗过度睡眠障碍。

LML134 Chemical Structure

Cas No.:1542135-76-1

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10mM (in 1mL DMSO)
¥2,602.00
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1mg
¥1,080.00
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5mg
¥3,150.00
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¥4,950.00
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¥8,910.00
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¥14,850.00
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产品描述

LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 is for the treatment of excessive sleep disorders[1].

LML134 (compound 18b) (oral; 10 mg/kg) indicates rapid oral absorption, with a Tmax of 0.5 hours, t1/2 of 1.54 hours and a fraction absorbed of 44%, as well as a rapid clearance in male Sprague-Dawley rats[1]. LML134 (i.v.; 1 mg/kg) has t1/2 of 0.44 hours, CL of 28 mL/min/kg and the low plasma protein binding in male Sprague-Dawley rat (Fu =39.0%)[1].

[1]. Troxler T, et al. The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders. ChemMedChem. 2019 Jul 3;14(13):1238-1247.

Chemical Properties

Cas No. 1542135-76-1 SDF
Canonical SMILES O=C(OC1CCN(C2=NN(C)C(C=C2)=O)CC1)N3CCN(C4CCC4)CC3
分子式 C19H29N5O3 分子量 375.47
溶解度 DMSO: 12.5 mg/mL (33.29 mM) 储存条件 Store at -20°C
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1 mM 2.6633 mL 13.3166 mL 26.6333 mL
5 mM 0.5327 mL 2.6633 mL 5.3267 mL
10 mM 0.2663 mL 1.3317 mL 2.6633 mL
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Research Update

The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders

ChemMedChem 2019 Jul 3;14(13):1238-1247.PMID:30957954DOI:10.1002/cmdc.201900176

Histamine H3 receptor (H3R) inverse agonists that have been in clinical trials for the treatment of excessive sleep disorders, have been plagued with insomnia as a mechanism-based side effect. We focused on the identification of compounds that achieve high receptor occupancy within a short time, followed by rapid disengagement from the receptor, a target profile that could provide therapeutic benefits without the undesired side effect of insomnia. This article describes the optimization work that led to the discovery of 1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate (18 b, LML134).