LML-134

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LML-134 是组胺 3 受体 (H3R)（hH3R cAMP 和 hH3R bdg，Kis 分别为 0.3 nM 和 12 nM）的反向激动剂。

LML-134 is an inverse agonist of Histamine 3 receptor (H3R)(hH3R cAMP and hH3R bdg with Kis of 0.3 nM and 12 nM). (In Vivo):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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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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GPCR/G Protein

Histamine Receptor

H3 receptor

Nervous system

Circadian Rhythm Disorders

1542135-76-1

375.47

C19H29N5O3

>98% (HPLC)

DMSO:7.5 mg/ml(19.97 mM; Need ultrasonic)

Cn1nc(ccc1=O)N1CCC(CC1)OC(=O)N1CCN(CC1)C1CCC1

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(-20℃)

With Ice Pack

≥ 2 years