LML-134
LML-134 Basic information
- Product Name:
- LML-134
- Synonyms:
-
- LML-134
- 1-Piperazinecarboxylic acid, 4-cyclobutyl-, 1-(1,6-dihydro-1-methyl-6-oxo-3-pyridazinyl)-4-piperidinyl ester
- inhibit,LML134,LML 134,Inhibitor,Histamine Receptor
- LML134, 10 mM in DMSO
- CAS:
- 1542135-76-1
- MF:
- C19H29N5O3
- MW:
- 375.47
- Mol File:
- 1542135-76-1.mol
LML-134 Chemical Properties
- Boiling point:
- 509.1±60.0 °C(Predicted)
- Density
- 1.37±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: 12.5 mg/mL (33.29 mM)
- pka
- 7.49±0.70(Predicted)
- form
- Solid
- color
- Light yellow to yellow
LML-134 Usage And Synthesis
Uses
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[1].
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[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].
IC 50
H3 receptor
References
[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. DOI:10.1002/cmdc.201900176
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