- 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 has the potential for excessive sleep disorders
- 靶点： H3 receptor
- 体内研究： 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. 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%)
- 参考文献：
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.
- 溶解性： Soluble in DMSO
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.663 ml 13.317 ml 26.633 ml 5 mM 0.533 ml 2.663 ml 5.327 ml 10 mM 0.266 ml 1.332 ml 2.663 ml 50 mM 0.053 ml 0.266 ml 0.533 ml
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
