产品
编 号:F182751
分子式:C19H29N5O3
分子量:375.47
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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25mg
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生物活性:
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.

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%).
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