LML-134
Catalog No: 2051510
CAS Number: 1542135-76-1
Purity: 98%
LML134 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.
For research use only. We do not sell to patients.
Chemical Information
| Name | LML-134 |
|---|---|
| Iupac Chemical Name | 1-(1-methyl-6-oxo-1,6-dihydropyridazin-3-yl)piperidin-4-yl 4-cyclobutylpiperazine-1-carboxylate |
| Synonyms | LML-134 ; LML 134 ; LML134 |
| Molecular Formula | C19H29N5O3 |
| Molecular Weight | 375.473 |
| Smile | O=C(N1CCN(C2CCC2)CC1)OC3CCN(C(C=C4)=NN(C)C4=O)CC3 |
| InChiKey | BVUJMFFRMZRNAT-UHFFFAOYSA-N |
| InChi | InChI=1S/C19H29N5O3/c1-21-18(25)6-5-17(20-21)23-9-7-16(8-10-23)27-19(26)24-13-11-22(12-14-24)15-3-2-4-15/h5-6,15-16H,2-4,7-14H2,1H3 |
| CAS Number | 1542135-76-1 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid |
|---|---|
| Purity | 98% |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | Avoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation. |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
| Targets | H3 receptor |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | LML134 (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%). |
| Clinical study | NCT02334449 Novartis Pharmaceuticals|Novartis Healthy Volunteers February 2015 Phase 1 NCT03141086 Novartis Pharmaceuticals|Novartis Circadian Rhythm Disorders July 26, 2017 Phase 2 |
Troxler T, Feuerbach D, Zhang X, et al. The Discovery of LML134, a Histamine H3 Receptor Inverse Agonist for the Clinical Treatment of Excessive Sleep Disorders. ChemMedChem. 2019;14(13):1238–1247. doi:10.1002/cmdc.201900176
Chemical Structure
