LML134 |
| Catalog No.GC38450 |
LML134(화합물 18b)는 hH3R cAMP 및 hH3R bdg에 대해 Kis가 0.3nM 및 12nM인 경구 활성 및 고선택성 히스타민 3 수용체(H3R) 역 효능제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1542135-76-1
Sample solution is provided at 25 µL, 10mM.
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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.
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